bluuebunny/crossref_metadata_2025 huggingface dataset:
Survival and Histopathological Study of Animals Bearing EhrlichTumor Treated With a Rhodium(II) Amidate
Authors: Espósito Breno Pannia , Zyngier Szulim Ber , Najjar Renato , Paes Roberto Pinto , Ueda Suely M. Ykko , Barros José Carlos A.
Published: March 2007

The survival of 90% of a tumor‐bearing population treated with the complex
was
examined and the pharmacological parameter Surv90
determined. Histopathological alterations raised for this
drug in several tissues were studied in Balb‐c mice. A Surv90
dose of 3.8x 10−5
mol/kg was found.
Toxicity of Certain Penta‐Coordinated Organotin(IV) andTetra‐Coordinated Tin(II) Complexes of Heterocyclic β–Diketones Against the Larvae of Aedes Aegypti (Liston)
Authors: Jain Asha , Saxena Sanjiv , Rai Audhesh K. , Saxena Prabhu N. , Rao J. Venkateshwara
Published: March 2007

Some organotin(IV) and tin(II) complexes of composition
(where R = C4H9, R′ = CH3
, C3H5
,p‐Cl C6H4
; R = C6H5

, R′ = C6H5
and p‐ClC6H4
) and
were screened for their toxicity against Aedes aegypti larvae.
Organotin(IV) complexes were more active than tin(II) complexes.
Biologically Active Transition Metal Chelates of Ni(II), Cu(II)and Zn(II) With 2‐Aminothiazole‐Derived Schiff‐bases: TheirSynthesis, Characterization and the Role of Anions (NO3, SO42−, C2O42- andCH3CO2−) on Their Antibacterial Properties
Authors: Chohan Zahid H.
Published: March 2007

Biologically active nickel(ll), copper(ll) and zinc(ll) chelates with thiazole‐derived nitro‐ and
chlorosalicylaldehyde Schiff‐bases having the same metal ion but different anions, e.g. nitrate,
sulfate, oxalate and acetate have been synthesized and characterized on the basis of their physical,
spectral and analytical data. In order to evaluate the possible participating role of anions on the
antibacterial properties, these ligands and their synthesized metal chelates with various anions have
been screened against bacterial species Escherichia coli, Pseudomonas
aeruginosa and Staphylococcus aureus.
Water Soluble Cyclophosphamide Adducts of Rhodium(II) Keto‐Gluconate and Glucuronate. Synthesis, Characterization and In Vitro Cytostatic Assays
Authors: Gil Eric de Souza , Gonçalves Maria Inês de Almeida , Ferreira Elizabeth Igne , Zyngier Szulin Ber , Najjar Renato
Published: March 2007

The synthesis, characterization and biological assays of two new rhodium carboxylate sugar derivatives and
respective cyclosphosphamide adducts are described. The compounds, characterized by  13C
and  1H NMR
,
infrared and UV‐visible spectra, presented high water solubility and hydration grades were confirmed given the
concordance between thermal and CHN analyses. The adducts were active in vitro against K‐562 cells.
Electronic Properties of Gold(I) Compounds Relevance to ChemicalReactions
Authors: Fackler John P. , Assefa Zerihun , Forward Jennifer M. , Grant Tiffany A.
Published: March 2007

The chemical reactivity of Au(I)compounds is related to their HOMO‐LUMO energy separation. For
coordinately unsaturated complexes of Au(I), the excited state (HOMO‐LU_MO separation) is only about 2 eV
above the ground state. Many Au(I)complexes such as [Au(TPPTS)3]8- and [Au(TPA)3]+ show visible luminescence from this state even in water solution. Quenching of the phosphorescence relates to the rate of
reaction ofthe substrate with the gold complex. Dioxygen and radicals such as NO rapidly react with the
Au(I) to quench the excited state, as do halocarbons capable of electron and/or atom transfer. Although
Corey and Khan suggested that a plausible mechanism for gold drug behavior in treatment for rheumatoid
arthritis, RA, might be quenching of singlet oxygen, our work demonstrates that NO and (which leads to
sh‐glet oxygen) each react rapidly to quench emission from Au(I). Drug action may relate to the prevention of
build‐up in cells by Au(I) of reactive, cytotoxic peroxynitrite, O2NO-q, formed quickly from and NO in
cells.
Spectroscopic Studies of Copper and Silver Binding toMetallothioneins
Authors: Stillman Martin J.
Published: March 2007

Mammalian metallothionein is remarkable in its metal binding properties: well‐characterized species exist for metal to sulfur ratios of M7S20, M12S20, and M18S20, where M = Cd(ll), Zn(ll), Hg(ll), Ag(I), Au(I), and Cu(I). Circular dichroism and luminescence spectra provide rich details of a complicated metal binding chemistry when metals are added directly to the metal free‐ or zinc‐containing protein. CD spectral data unambiguously identify key metal to protein stoichiometric ratios that result in well‐defined structures. Emission spectra in the 450‐750 nm region have been reported for metallothioneins containing Ag(I), Au(I), and Cu(I). The luminescence of Cu‐MT can also be detected directly from mammalian and yeast cells. Qualitative and quantitative interpretations show that the final structure adopted by Ag‐MT is not the same as that formed by Cu(I) ions in Cu‐MT. XAFS structural data are reported for a number of metallothioneins, including Ag12‐MT and Ag17‐MT. Electrospray ionization mass spectrometry provides details on the species formed when Ag(I) binds to metallothionein. Mass spectral data are reported for metal‐free MT 2A and Agn‐MT (n = 14‐18).
Characterisation and In Vitro Cytotoxicity ofTriorganophosphinegold(I) 2‐Mercaptobenzoate Complexes
Authors: de Vos Dick , Clements Phil , Pyke Simon M. , Smyth Douglas R. , Tiekink Edward R. T.
Published: March 2007

The preparation and full NMR ( 1H, 13C and  31P)
characterisation of three R3PAu
(2mba)
complexes, Where R = Et, Ph and Cy, and 2mba is the anion derived from 2‐mercaptobenzoic acid
is reported. An interesting solvent dependence in the 1H spectra is rationalised in terms of
competing intra‐ and inter‐molecular hydrogen bonding. An X‐ray analysis of the [Ph3PAu(2mba)]

species reveals a linear P—Au—S arrangement and association in the lattice via the familar carboxylic acid dimer motif. The in Vitro cytotoxicity against seven human tumout lines is also
described. The complexes display moderate to very high activity. Particularly noteworthy is their greater activity against the H226 cell line (non‐small cell lung cancer) compared with that displayed
by a range of cytotoxic drugs.
Silver Ions in the Treatment of Local Infections
Authors: Becker Robert O.
Published: March 2007

A study of the use of free silver ions as an antibacterial and antifungal agent administered to
infected local wounds has been conducted over the past two decades. A variety of iontophoretic
techniques has been employed utilizing either pure silver wires or several types of silvered nylon
fabrics as anodes in a direct current electrical circuit. A new type of silver nylon has recently been
evaluated for the same use without iontophoretic current. In vitro studies of both techniques have
demonstrated an effective, broad spectrum antibiotic effect including most silver‐resistant strains.
Over 100 cases of recalcitrant osteomyelitis have been treated with an overall success rate of
approximately 65% and no evidence of argyria.
Metal Ion‐Binding Properties of the Diphosphate Ester Analogue,Methylphosphonylphosphate, in Aqueous Solution
Authors: Song Bin , Zhao Jing , Gregáň Fridrich , Prónayová Nadja , Sajadi S. Ali A. , Sigel Helmut
Published: March 2007

The stability constants of the 1:1 complexes formed between methylphosphonylphosphate
, and Mg2+, Ca2+, Sr2+, Ba2+, Mn2+, Co2+, Ni2+, Cu2+, Zn2+,​ or Cd2+ (M2+)
were determined by potentiometric pH titration in aqueous solution (25  °C
; l = 0.1 M,
NaNO3
). Monoprotonated M(H;MePP) complexes play only a minor role. Based on previously
established correlations for M2+
‐diphosphate monoester complex‐stabilities and diphosphate
monoester β‐group. basicities, it is shown that the M(Mepp) -
complexes for Mg2+
and the ions of
the second half of the 3d series, including Zn2+
and Cd2+, are on average by about 0.15 log unit
more stable than is expected based on the basicity of the terminal phosphate group in MePP3-. In contrast, Ba(Mepp) -
and Sr(Mepp) -
are slightly less stable, whereas the stability for Ca(Mepp) -
is
as expected, based on the mentioned correlation. The indicated increased stabilities are explained
by an increased basicity of the phosphonyl group compared to that of a phosphoryl one. For the
complexes of the alkaline earth ions, especially for Ba2+, it is suggested that outersphere
complexation occurs to some extent. However, overall the M(Mepp) -
complexes behave rather as
expected for a diphosphate monoester ligand.
The Hypolipidemic and Anti‐Inflammatory Activity of BoronatedAromatic Amino Acids in CF1 Male Mice
Authors: Miller Merrill C. , Sood A. , Spielvogel Bernard F. , Hall Iris H.
Published: March 2007

The boronated aromatic amino acids were shown to be potent hypolipidemic agents in mice lowering both
serum cholesterol and triglycerides after 16 days. Selective compounds were as effective as the clinical
standards. Furthermore, the compounds were effective anti‐inflammatory agents reducing local and central pain
as well as suppressing LPS induced endotoxic shock in mice. These agents inhibited lysosomal and
proteolytic enzymes of the liver and macrophages as a part of their mechanism of action.
Synthesis, Characterisation and Anti‐Fungal Activities of Some NewCopper(II) Complexes of Octamethyl Tetraaza‐Cyclotetradecadiene
Authors: Roy Tapashi G. , Hazari Saroj K. S. , Dey Benu K. , Chakraborti Samar , Tiekink Edward R. T.
Published: March 2007

The ligand Me8[14]diene, L, in its free state as well as in the dihydroperchlorate form,
L.2HClO4, coordinates copper(ll) in different salts to yield a series of
complexes
where X = NO3, ClO4, NCS, Cl and Br; x and y may have values of 0 or 2 and z = 0, 1 or 2. The
complex,
is found to undergo axial ligand substitution reactions with SCN-
,
and Cl- to give a variety of substitution derivatives:
where X = NCS, NO3
and Cl; m = 0 or 1, and n = 1 or 2. The complexes .have been characterised on the basis of analytical,
spectroscopic, magnetic and conductance data. The anti‐fungal activities of the ligand and its
complexes have been investigated against a range of phytopathogenic fungi.
Binding of Platinum(II) to Some Biologicaly Important Thiols
Authors: Petrovic Biljana V. , Djuran Milos I. , Bugarcic Zivadin D.
Published: March 2007

The reactions between [Pt(terpy)Cl+
and thiols, such as glutathione, L‐cysteine,
D‐penicillamine and thioglycolic acid have been Studied by conventional UV‐VIS spectrophotometry and H
NMR spectroscopy. The second‐ordero rate constants, K2, are similar for these four thiols, varying between
1.06 x 10−2
and 6.10 x 10−3 M-1s-1
at 25  °C
. The activation entropies have large negative values between ‐100
and ‐200 J mol-1
which are compatible with an associative A mechanism. However, L‐methionine, as
thioether ligand, is unreactive under the same experimental conditions. The obtained results have been
analyzed in relation to the antitumor activity and toxicity of platinum(II) complexes.
Carbonic Anhydrase Inhibitors Part 721 Synthesis and AntiglaucomaProperties of Metal Complexes of p‐Fluorobenzolamide
Authors: Supuran Claudiu T. , Scozzafava Andrea , Menabuoni Luca , Mincione Francesco , Briganti Fabrizio , Mincione Giovanna
Published: March 2007

Metal complexes of a heterocyclic sulfonamides possessing very strong carbonic anhydrase (CA)
inhibitory properties, i.e., 5‐(p‐fluorobenzenesulfonylamido)‐1,3,4‐thiadiazole‐2‐sulfonamide (p‐fluorobenzolamide)
were prepared. The new complexes contained metal ions such as Zn(II), Cu(II), Co(II), Ni(II),
Cd(II) and Mn(II). The new compounds were characterized by standard physico‐chemical procedures, and
assayed as inhibitors of three CA isozymes, CA I, II and IV. Very good inhibition has been evidenced both
for the parent sulfonamides as well as for the prepared complexes, against all three investigated isozymes.
Some of these new complexes as well as the parent sulfonamide, strongly lowered intraocular pressure (IOP)
in normotensive rabbits when administered as a 2% solution into the eye.
Biological Role of Anions (Sulfate, Nitrate , Oxalate and Acetate)on the Antibacterial Properties of Cobalt (II) and Nickel(II)Complexes With Pyrazinedicarboxaimide Derived, Furanyl and ThienylCompounds
Authors: Chohan Zahid H. , Praveen M.
Published: March 2007

A number of biologically active complexes of cobalt(II) and nickel(II) with pyrazinedicarboxaimido derived
thienyl and furanyl compounds having the same metal ion but different anions such as sulphate, nitrate,
oxalate and acetate have been synthesized and characterized on the basis of their physical, spectral and
analytical data. In order to evaluate the role of anions on their antibacterial properties, these ligands and
their synthesized metal complexes with various anions have been screened against bacterial species
Escherichia coil,Pseudomonas aeruginosa and Staphylococcus aureus. The title studies have proved a definitive role of anions in increasing the antibacterial properties.
Hydroxynaphthoquinone Metal Complexes as Antitumor Agents X: Synthesis, Structure, Spectroscopy and In Vitro Antitumor Activity of 3‐Methyl‐Phenylazo Lawsone Derivatives and Their Metal Complexes Against Human Breast Cancer Cell Line MCF‐7
Authors: Gokhale Nikhil , Padhye Subhash , Newton Chris , Pritchard Robin
Published: March 2007

The C‐3 substituted phenylazo derivatives of lawsone (2‐hydroxy‐l,4 p‐naphthoquinone, III) were synthesized and characterized. The X‐ray crystal structure was determined for the ligand 3‐(3′‐methyl phenylazo) lawsone. The copper complexes of these derivatives were found to possess 1:2 metal stoichiometry and square planar geometries with intermolecular stackings, resulting in antiferromagnetic exchange interactions. The in vitro activity of all the synthesized compounds was examined against human breast cancer cell‐line, MCF‐7, which revealed enhanced activities for the metal complexes, the highest activity being observed for the copper compound of 3‐(3′‐methyl phenylazo) lawsone.
Preparation and Crystal Structure of a Rhenium Analogue of the Cationic Renal Agent, Tc‐99m Diaminocyclohexane
Authors: Marzilli Luigi G. , Hansen Lory , Taylor Andrew , Lachicotte Rene
Published: March 2007

We report here a chemical study on a Re analogue of one of the few cationic Tc‐99m tracers previously investigated as an agent for effective renal plasma flow (ERPF) measurement. Cationic Tc‐99m tracers have the potential for overcoming problems associated with common anionic Tc‐99m tracers in patients who have developed a uremic state. The Tc‐99m‐DACH tracer, prepared from 1,2‐diaminocyclohexane (1,2‐DACH), is the only cationic renal agent tested in humans and has seven possible isomers. The complex isolated from the reaction of the racemic mixture, (±)‐trans‐1,2‐DACH, and ReIO2(PPh3)2 after conversion to the BPh4- salt was found by X‐ray crystallography to be the meso isomer, trans‐[ReO2 (trans-R,R‐1,2‐DACH)(trans-S,S‐l,2‐DACH)][BPh4]·MeOH · 2H2O (1). The structural parameters for 1 are normal. The complex is highly symmetrical, suggesting that the analogous meso Tc‐99m‐DACH agent is also symmetrical. Studies of other Tc‐99m‐DACH agents that were made from cis‐1,2‐DACH or individual trans‐1,2‐DACH enantiomers show that the biodistribution is not very dependent on the starting 1,2‐DACH ligand stereochemistry; these agents must be less symmetrical than the meso Tc‐99m‐DACH agent analogue of 1. Thus, the overall charge and lipophilicity (similar for all Tc‐99m‐DACH isomers) exert a greater influence on biodistribution than the specific structural features of the different Tc‐99m‐DACH isomers.
Effects of a Single Venous Dose of Zinc on Thyroid Status in Healthy Individuals and Patients With Graves′ Disease
Authors: Farooqi Lubna , Mazeto Gláucia M. F. S. , Shuhama Tadao , Brandão-Neto José
Published: March 2007

Zinc metabolism may regulate thyroid function acting at TRH (thyrotropin‐releasing hormone) synthesis, peripheral deiodination of T4 (tetraiodothyronine), and binding of thyroid hormones to nuclear receptors. The aim of this study was to investigate the effect of acute zinc administration on TSH (thyroid‐stimulating hormone), FT3 (free triiodothyronine), and FT4 (free tetraiodothyronine) in 10 healthy individuals and 12 hyperthyroid patients with Graves′ disease. All these individuals were studied following 25 mg Zn++ administered intravenously, at 7:00 a.m. after 12 h fast. Blood samples collected at 0, 3, 30, 60, 90, and 120 min after zinc administration showed no significant alteration in the plasma levels of TSH, FT3, and FT4 in hyperthyroid patients. There were no changes in the plasma levels of FT3 and FT4 in the control subjects, but TSH levels were acutely depressed by zinc administration. This study suggests that zinc given acutely and in pharmacological doses does not affect thyroid function in hyperthyroid subjects, but affect plasma TSH levels in healthy individuals.
Insulin Mimetic Peroxo Complexes of Vanadium Containing Uracil or Cytosine as Ligand
Authors: Sarkar Asit R. , Mandal Shipra
Published: March 2007

Mixed ligand oxo peroxo complexes of vanadium (V), M[VO(O2)L2].nH2O where M = K or NH4, HL = uracil or cytosine and n = 1 or 2, have been isolated from aqueous methanolic medium. The complexes were characterised by elemental analysis, conductance, TGA, UV‐Visible, IR and NMR spectral studies. Both the peroxide and the other ligands acts as chelates coordinating through their oxygen at C (2) and nitrogen at N (3) and the presence of monomeric oxoperoxovanadium (V) species, have been established by IR,  1H and  51V NMR studies. The complexes appeared to possess pentagonal bipyramidal geometry. The terminal oxo ligand and the oxygen of the uracil or cytosine at C (2) occupy the axial position while the peroxide and the other donor ligands are in the equatorial position. The UV spectral studies confirm the presence of Vanadium in its +5 oxidation state. The administration of the potassium salts of the complexes reduces the blood glucose level in Swiss Albino mice compared to that of KVO3. The complexes also readily oxidise cysteine to Cystine in aqueous solution. The possible mechanism for the insulin‐mimic activity of the complexes is discussed.
Synthesis, Characterization and Biological Properties of Tridentate NNO, NNS and NNN Donor Thiazole‐Derived Furanyl, Thiophenyl and Pyrrolyl Schiff Bases and Their Co(II), Cu(II), Ni(II) and Zn(II) Metal Chelates
Authors: Chohan Zahid H. , Kausar Samina
Published: March 2007

2‐Aminothiazole undergoes condensation reactions with furane‐, thiophene‐ and pyrrole‐2‐carboxylaldehyde to give tridentate NNO, NNS and NNN Schiff bases respectively. These tridentate Schiff bases formed complexes of the type [M (L) 2]X2 where [M=Co(II), Cu(II), Ni(II) or Zn(II), L=N‐(2‐furanylmethylene)‐2‐aminothiazole (L1), N‐(2‐thiophenylmethylene)‐2‐aminothiazole (L2), N‐(2‐pyrrolylmethylene)‐2‐aminothiazole (L3) and X=Cl. The structures of these Schiff bases and of their complexes have been determined on the basis of their physical, analytical and spectral data. The screening results of these compounds indicated them to possess excellent antibacterial activity against tested pathogenic bacterial organisms e.g., Escherichia coli, Staphylococcus aureous and Pseudomonas aeruginosa. However, in comparison, their metal chelates have been shown to possess more antibacterial activity than the uncomplexed Schiff bases.
Insights Into the Mode of Action of the Anti‐Candida Activity of 1,10‐Phenanthroline and its Metal Chelates
Authors: McCann Malachy , Geraghty Majella , Devereux Michael , O′Shea Denis , Mason James , O′Sullivan Luzveminda
Published: March 2007

Metal complexes of malonie acid (metal = Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Ag(I)) were
prepared and only the Ag(I) complex inhibited the growth of Candida albicans. Malonate complexes
incorporating the chelating 1,10‐phenanthroline (1,10‐phen) ligand showed a range of activities: good
(Mn(II), Cu(II), Ag(I)); moderate (Zn(II)); poor (Co(II), Ni(II)). Metal‐free 1,10‐phen and Ag(CH3CO2)
were also highly active. The metal‐free non‐chelating ligands 1,7‐ phenanthroline and 4,7‐phenanthroline
were inactive and the Cu(II), Mn(II) and Zn(II) complexs of 1,7‐phen displayed only marginal activity.
Whereas the Cu(II) malonate/1,10‐phen complex induces significant cellular oxidative stress the Zn(II)
analogue does not.
Isolation, Characterization and Antitumour Propirties of the 1,2‐Popylenediaminetetraacetate trans‐Diaqua‐Copper (II)
Authors: Kamah S. , Vilaplana R. , Moreno J. , Akdi K. , García-Herdugo G. , González-Vílchez F.
Published: March 2007

A trans‐diaquacomplex formed by copper(II) sulphate and the sequestering polyamminopolycarboxylic
ligand 1,2‐propylenediaminetetraacetic acid (PDTA) has been isolated and characterized by
chemical analysis, titrimetry, FT‐IR and electronic spectroscopy, Potentiometric and electronic
measurements identified the ligand as tetradentate, two nitrogen and two oxygen atoms being bonded to the
Cu(II) in planar positions. This octahedral monomeric soluble compound, is an unusual example of a copper
(II) substance showing significant in vitro antitumour activity against the human ovarian tumour cells TG
(ID50 = 2.29 μM at 48 h) and important in vivo antitumour activity against solid Sarcoma 180 with
complete regression of the tumour at a dose of 12.5 mg/Kg body weight.
Solvolysis of the Tumor‐Inhibiting Ru(III)‐Complex trans‐Tetrachlorobis(Indazole)Ruthenate(III)
Authors: Pieper Thomas , Peti Wolfgang , Keppler Bernhard K.
Published: March 2007

The ruthenium(III) complex Hlnd trans‐[RuCl4,(ind)2], with two trans‐standing indazole (ind)
ligands bound to ruthenium via nitrogen, shows remarkable activity in different tumor models
in vitro and in vivo. The solvolysis of the complex trans‐[RuCl4,(ind)2]- has been investigated by means of spectroscopic techniques (UV/vis, NMR)in different solvents. We investigated the
indazolium as well as the sodium salt, the latter showing improved solubility in water. In
aqueous acetonitrile and ethanol the solvolysis results in one main solvento complex. The
hydrolysis of the complex is more complicated and depends on the pH of the solution as well
as on the buffer system.
Antitumor Trans Platinum DNA Adducts: NMR and HPLC Study of the Interaction Between a trans‐Pt Iminoether Complex and the Deoxy Decamer d(CCTCGCTCTC)·d(GAGAGCGAGG)
Authors: Andersen Bjørn , Margiotta Nicola , Coluccia Mauro , Natile Giovanni , Sletten Einar
Published: March 2007

The single‐stranded oligonucleotide 5′‐d(CCTCGCTCTC) (I) was reacted with the antitumor trans platinum iminoderivative trans‐[PtCl2{E‐HN = C(OMe)Me}2] (trans-EE) and subsequently annealed with its complementary strand 5′‐d(GAGAGCGAGG) (II). The platinated duplex was characterized by 1D and 2D proton NMR spectroscopy at 600 MHz. In agreement with previous studies by different techniques trans-EE was found to form a monofunctional adduct with the duplex involving the guanine residue. The modification by trans-EE has been found to induce only minor local distortion in the duplex geometry. Two key crosspeaks observed in the NOESY map corresponding to a close contact between G5‐H8 and the methoxy and the methyl group, respectively, enabled us to dock the trans-EE complex with the duplex by geometry optimization. The results support the idea that the antitumor activity of trans-EE is related to lesion of DNA fundamentally different from that of cisplatin. Unexpectedly, the NOESY spectra indicated that at the high NaCl concentration used (0.2 M) the duplex was found to undergo slow deplatination. This was subsequently proved by HPLC. In a separate experiment on platination of the single strand in a salt free environment the HPLC analysis showed that the monofunctional adduct was not deplatinated, however, after 24 hours, additidnal minor isomers were detected.
Synthesis, Characterization and Antitumour Activity of Some Butyltin(IV) Cysteaminates and N,N‐Dimethylcysteaminates
Authors: Gielen Marcel , Handlir Karel , Hollein Martin , de Vos Dick
Published: March 2007

The synthesis and characterization of four di‐ and tri‐n‐butyltin cysteaminates and N,N‐dimethylcysteaminates and three protonated / quaternized derivatives are reported. They all exhibit moderate or high in vitro cytotoxic activity. Six of seven compounds presented in this work are more active than cisplatin, etoposide and 5‐fluorouracil, but less active than methotrexate and doxorubicin.
Comparative Analysis of [Au(en)2] 3+ and [Pt(en)2] 2+ non Covalent Binding to Calf Thymus DNA
Authors: Marcon Giordana , O′Connell Tim , Orioli Pierluigi , Messori Luigi
Published: March 2007

Reactions of the complexes bisethylendiammine gold(III) and bisethylendiammine platinum(II) with calfthymus DNA were comparatively analysed. Both complexes bind DNA non‐covalently most probably on the basis of electrostatic interactions. Binding of either complex at low ratios results into modest modifications of B‐type DNA conformations, as detected by CD. Far larger CD alterations are observed at high ratios. The gold(III) chromophore is scarcely perturbed by DNA addition Binding of [Au(en)2]Cl3 to calf thymus DNA is reversed by sodium cyanide. By analogy with the case of [Pt(en)2]Cl2 it is suggested that Auen acts as a minor groove binder.
Synthesis, Characterization and Biological Evaluation of Co(II), Cu(II), Ni(II) and Zn(II) Complexes With Cephradine
Authors: Chohan Zahid H. , Jaffery Maimoon F.
Published: March 2007

Some Co(II), Cu(II), Ni(II) and Zn(II) complexes of antibacterial drug cephradine have been prepared and characterized by their physical, spectral and analytical data. Cephradine acts as bidentate and the complexes have compositions, [M(L)2X2] where [M = Co(II), Ni(II) and Zn(II), L = cephradine and X = Cl2] showing octahedral geometry, and [M(L)2] where [M = Cu(II), L = cephradine] showing square planar geometry. In order to evaluate the effect of metal ions upon chelation, eephradine and its complexes have been screened for their antibacterial activity against bacterial strains, Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa.
Effects of Organoantimony(III) Compounds of Sterically Hindered Bifunctional Tetradentate Ligands on the Reproductive System of Male Rats
Authors: Sharma R. K. , Dobhal M. P. , Singh Y. P. , Rai A. K. , Sharma R. , Chaudhary R. , Yadav R. , Gupta R. S.
Published: March 2007

The antifertility activity of organoantimony(III) complexes PhSb[RC(NC6H4S)CH2(NC6H4S)CR′] {R′ = CH3 (R1) and R = R′ = CF3 (R2)} derived from corresponding sterically hinlered bifuinctional tetradentate ligands in the male rats was determined. The administration of compounds R1 and R2 at the dose level of 20 mg/kg. b. wt. siignificantly reduced the weights of testes and epididymides. Auxiliary glands showed a significant reduction after the treatment of compound R1 only. Treated animals showed a notable depression of spermatogenesis. The preleptotene spermatocytes were decreased by 76.19 and 47.06; the secondary spermatocytes by 87.4% and 54.87337; and the step‐19 spermatids by 72.9 and 46.77% respectively, following the compound R1 and R2 treatment. Reduced sperm count and motility resulted in 100% negative fertility in both the treated groups. A significant fall in the content of various biochemical parameters of eproductive tissues was observed after R1 and R2 treatment in comparison to controls.
Synthesis and Biological Activity of Manganese (II) Complexes of Phthalic and Isophthalic Acid: X‐Ray Crystal Structures of [Mn(ph)(Phen)2(H2O)]· 4H2O, [Mn(Phen)2(H2O)2]2(Isoph)2(Phen)· 12H2O and {[Mn(Isoph)(bipy)]4· 2.75biby}n(phH2 = Phthalic Acid; isoph = Isophthalic Acid; phen = 1,10‐Phenanthroline; bipy = 2,2‐Bipyridine)
Authors: Devereux Michael , McCann Malachy , Leon Vanessa , Geraghty Majella , McKee Vickie , Wikaira Jan
Published: March 2007

Manganese(II) acetate reacts with phthalic acid (phH2) to give [Mn(ph)]·0.5H2O (1). Reaction of 1 with 1,10‐phenanthroline produces [Mn(ph)(phen)]·2H2O (2) and [Mn(ph)(phen)2(H2O)]·4H2O (3). Reaction of isophthalic acid (isophH2) with manganese(II) acetate results in the formation of [Mn(isoph)]·2H2O (4). The addition of the N,N‐donor ligands 1,10‐phenanthroline or 2,2′‐bipyridine to 4 leads to the formation of [Mn2 (isoph)2(phen)3)]·4H2O (5), [(Mn(phen)2(H2O)2]2(isoph)2(phen)·12H2O (6) and {[Mn(isoph)(bipy)]4·2.75 biby}n (7), respectively. Molecular structures of 3, 6 and 7 were determined crystallographically. In 3 the phthalate ligand is bound to the manganese via just one of its carboxylate groups in a monodentate mode with the remaining coordination sites filled by four phenanthroline nitrogen and one water oxygen atoms. In 6 the isophthalates are uncoordinated with the octahedral manganese center ligated by two phenanthrolines and two waters. In 7 the Isophthalate ligands act as bridges resulting in a polymeric structure. One of the carboxylate groups is chelating a single manganese with the other binding two metal centres in a bridging bidentate mode. The phthalate and isophthalate complexes, the metal free ligands and a number of simple manganes salts were each tested for their ability, to inhibit the growth of Candida albicans. Only the “metal free” 1,10‐phenanthroline and its manganese complexes were found to be
active.
A Theoretical‐Experimental Study on the Structure and Activity of Certain Quinolones and the Interaction of Their Cu(II)‐Complexes on a DNA Model
Authors: Robles J. , Martín-Polo J. , Álvarez-Valtierra L. , Hinojosa L. , Mendoza-Díaz G.
Published: March 2007

Theoretical electronic Structure methods have been employed to study the structure and activity of certain (free) quinolones and the interaction of their Cu(II)‐complexes on a DNA model (Rhodamine 6G (rhod)). As a manner of assessing the generated geometries, the nalidixic acid geometrical parameters obtained were tested against the crystallographic ones and it was found that the average error in the calculated geometries is small. The present study allows us to (1) Rationalize the observed differences in antibiotic activities through their electronic hardnesses. (2) Suggest a plausible mechanism of action for these drugs through formation of a reactive intermediate (or carrier) which would consist of a quinolone anion coordinated to an adequate metal center (Cu(II) in this study). (3) We find that, through this model of DNA (modeled with rhod) the interaction seems to be mediated by an effective π‐π stacking. (4) Finally, an in vitro experiment was designed so that the intercalation process in DNA could be experimentally modeled as well. The quenching of the rhod fluorescence is proportional to the strength of the Cu(II)‐complex‐rhod interaction and therefore provides a quantitative measurement of the “intercalating” capacity of the quinolones and their copper complexes. These results agree well with the theoretical total adduct formation energies.
Ternary Copper(II) Complexes in Solution[1,2] Formed With 8‐Aza Derivatives of the Antiviral Nucleotide Analogue 9‐[2‐(Phosphonomethoxy)Ethyl]Adenine (PMEA)
Authors: Gómez-Coca Raquel B. , Kapinos Larisa E. , Holý Antonín , Vilaplana Rosario A. , González-Vílchez Francisco , Sigel Helmut
Published: March 2007

The stability constants of the mixed‐ligand complexes formed between Cu(Arm)2+, where Arm= 2,2′‐bipyridine (Bpy) or 1,10‐phenanthroline (Phen), and the dianions of 9‐[2‐(phosphonomethoxy)ethyl]‐8‐azaadenine (9,8aPMEA) and 8‐[2‐(phosphonomethoxy)ethyl]‐8‐azaadenine (8,8aPMEA) (both also abbreviated as PA2-) were determined by potentiometric pH titrations in aqueous solution (25 °C; I = 0.1 M, NaNO3). All four ternary Cu(Arm)(PA) complexes are considerably more stable than corresponding Cu(Arm)(R‐PO3) species, where R‐P represents a phosph(on)ate ligand with a group R that is unable to participate in any kind of interaction within the complexes. The increased stability is attributed to intramolecular stack formation in the Cu(Arm)(PA) complexes and also to the formation of 5‐membered chelates involving the ether oxygen present in the ‐CH2‐O‐CH2‐P residue of the azaPMEAs. A quantitative analysis of the intramolecular equilibria involving three structurally different Cu(Arm)(PA) species is carried out. For example, about 5% of the Cu(Bpy)(8,8aPMEA) system exist with the metal ion solely coordinated to the phosphonate group, 14% as a 5‐membered chelate involving the ‐CH2‐O‐CH2‐Presidue, and 81% with an intramolecular stack between the 8‐azapurine moiety and the aromatic rings of Bpy. The results for the other systems are similar though with Phen a formation degree of about 90% for the intramolecular stack is reached. The existence of the stacked species is also proven by spectrophotometric measurements. In addition, the Cu(Arm)(PA) complexes may be protonated, leading to Cu(Arm)(H;PA)+ species for which it is concluded that the proton is located at the phosphonate group and that the complexes are mainly formed by a stacking adduct between Cu(Arm)2+ and H(PA)-. Conclusions regarding the biological properties of these azaPMEAs are shortly indicated.
Chemistry and Pharmacokinetics of Gallium Maltolate, a Compound With High Oral Gallium Bioavailability
Authors: Bernstein Lawrence R. , Tanner Trevor , Godfrey Claire , Noll Bruce
Published: March 2007

Gallium maltolate, tris(3‐hydroxy‐2‐methyl‐4H‐pyran‐4‐onato)gallium (GaM), is an orally active gallium compound for therapeutic use. It is moderately soluble in water (10.7 ± 0.9 mg/mL at 25 ∘C) with an octanol partition coefficient of 0.41±0.08. The molecule is electrically neutral in aqueous solution at neutral pH; a dilute aqueous solution (2.5 ×10−5 M) showed little dissociation at pH 5.5‐8.0. Single crystal X‐ray diffraction analysis found the GaM molecule to consist of three maltolate ligands bidentately bound to a central gallium atom in a propeller‐like arrangement, with one of the ligands disordered in two possible orientations. The compound is orthorhombic, space group Pbca, unit cell a = 16.675(3), b = 12.034(2), c = 18.435(2) at 158K. GaM was administered to healthy human volunteers at single doses of 100, 200, 300, and 500 mg (three subjects per dose). GaM was very well tolerated. Oral absorption of Ga into plasma was fairly rapid (absorption half life = 0.8‐2.0h), with a central compartment excretion half life of 17‐21h. Absorption appeared dose proportional over the dosage range studied. Estimated oral gallium bioavailability was approximately 25‐57%, based on comparison with published data on intravenous gallium nitrate. Urinary Ga excretion following oral GaM administration was approximately 2% of the administered dose over 72h, in contrast to 49‐94% urinary Ga excretion over 24h following i.v. gallium nitrate administration. We suggest that oral administration of GaM results in nearly all plasma gallium being bound to transferrin, whereas i.v. administration of gallium nitrate results in formation of considerable plasma gallate [Ga], which is rapidly excreted in the urine. These data support the continued investigation of GaM as an orally active therapeutic gallium compound.
Binding of Antitumor Ruthenium(III) Complexes to Plasma Proteins
Authors: Messori L. , Vilchez F. Gonzales , Vilaplana R. , Piccioli F. , Alessio E. , Keppler B.
Published: March 2007

Presently, there is large interest in analysing the interactions in vitro with plasma proteins of some novel antitumor ruthenium(III) complexes that are in preclinical or clinical phase. The joint application of separation and spectroscopic techniques provides valuable information on the nature and the properties of the resulting ruthenium/protein adducts. Recent work carried out in our laboratory points out that, under physiological conditions, some selected ruthenium(III) complexes bind plasma proteins tightly with a marked preference for surface imidazole groups. Representative examples of interactions of antitumor ruthenium(III) complexes with plasma proteins such as albumin and transferrin are given. Notably the antitumor ruthenium(III) complexes considered here bind proteins much tighter than DNA; it is proposed that protein binding of ruthenium(III) complexes will have a large impact on the biodistribution, the pharmacokinetics and the mechanism of action of these experimental drugs.
Synthesis, Characterization and Antitumor Activity of a Series of Polypyridyl Complexes
Authors: Liu Jie , Zou Xiao-Hua , Zhang Qian-Ling , Mei Wen-Jie , Liu Jian-Zhong , Ji Liang-Nian
Published: March 2007

A series of polypyridyl complexes have been synthesized. All polypyridyl complexes and some of the soluble ligands have been assayed for antitumor activity in vitro against the HL‐60 (the human leucocytoma) cells, BEL‐7402 (the human liver carcinoma) cells, KB (the human nasopharyngeal carcinoma) cells and HELA (the human adenocarcinoma of cervix) cells. The results indicate that several complexes have relative activity against different cell lines. Especially, the complexes [Co(bpy)2(pip)]3+, [Co(phen)2(pip)]3+, [Ru(bpy)2(pztp)]2+ and [Ru(pztp)2(bpy)]2+ show relative high activity against four tumor cell lines. Moreover, they are slightly more effective than cisplatin. At the concentration of 100 μg/mL, the complexes show inhibitory rate of 72∼86% for the cancer cells and have no toxicity for MDCK and Vero cells. It is indicated that these complexes can inhibit cancer cells selectively.
Antifungal Activity of Ag(I) and Zn(II) Complexes of Sulfacetamide Derivatives
Authors: Mastrolorenzo Antonio , Supuran Claudiu T.
Published: March 2007

Reaction of sulfacetamide with arylsulfonyl isocyanates afforded a series of derivatives which were used as ligands (as conjugate bases) for the preparation of metal complexes containing Ag(I) and Zn(II). The newly synthesized complexes, unlike the free ligands, act as effective antifungal agents against Aspergillus and Candida spp., some of them showing activities comparable to ketoconazole, with minimum inhibitory concentrations in the range of 0.3 – 0.5 μg/mL. The mechanism of antifungal action of these complexes seems to be not connected with the inhibition of lanosterol‐14‐α‐demethylase, since the levels of sterols assessed in the fungi cultures were equal in the absence or in the presence of the tested compounds. Probably the new complexes act as inhibitors of phosphomannose isomerase, a key enzyme in the biosynthesis of yeast cell walls.
Carbonic Anhydrase Inhibitors. Part 91. Metal Complexes of Heterocyclic Sulfonamides as Potential Pharmacological Agents in the Treatment of Gastric Acid Secretion Imbalances
Authors: Ilies Marc A. , Supuran Claudiu T. , Scozzafava Andrea
Published: March 2007

Zinc, magnesium, aluminum and copper complexes of several potent, clinically used carbonic anhydrase (CA) sulfonamide inhibitors, such as acetazolamide, methazolamide, ethoxzolamide and benzolamide were tested for their possible applications as antacids, in experimental animals. Gastric acid secretion parameters 3 days after treatment with these CA inhibitors (2 × 500 mg, twice a day), in dogs with chronic gastric fistulas, led to the observation that the gastric acid parameters BAO (the basal acid output), and MAO (the maximal acid output after stimulation with histamine) were drastically reduced, as compared to the same parameters in animals that did not receive these enzyme inhibitors. These are promising results for the possible use of metal complexes of heterocyclic sulfonamides as treatment alternatives (alone or in combination with other drugs) for gastric acid secretion imbalances.
Cytotoxic Activity of Silyl‐ and Germyl‐Substituted 4,4‐Dioxo‐3a,6a‐Dihydrothieno[2, 3 − d]isoxazolines‐2
Authors: Lukevics E. , Arsenyan P. , Shestakova I. , Zharkova O. , Kanepe I. , Mezapuke R. , Pudova O.
Published: March 2007

The [2+3] dipolar cycloaddition of nitrile oxides to the double C = C bonds of thiophene‐1, 1‐dioxides leads to formation of the fused isoxazolines‐2 (1, 2). Tumor growth inhibition of these compounds strongly depends on the nature of group IV A element increasing from slightly active tert-butyl derivatives to silicon and germanium containing analogues. The products of benzonitrile oxide cycloaddition have greater cytotoxic effect than the compounds obtained from the cycloaddition reaction of 2, 5‐disubstituted thiophene‐1, 1‐dioxides with acetonitrile oxide. Fused silyl substituted isoxazolines‐2 are stronger NO‐inducers than their germyl and tert-butyl analogues.
Developing Carrier Complexes for “Caged NO”: RuCl3(NO)(H2O)2 Complexes of Dipyridylamine, (dpaH), N,N,N′N′‐Tetrakis (2‐Pyridyl) Adipamide, (tpada), and (2‐Pyridylmethyl) Iminodiacetate, (pida2-)
Authors: Slocik Joseph M. , Kortes Richard A. , Shepherd Rex E.
Published: March 2007

Delivery agents which can carry the {Ru(NO)} 6 chromophore (“caged NO”) are desired for vasodilation and for photodynamic therapy of tumors. Toward these goals, complexes derived from (1) have been prepared using dipyridylamine (dpaH) as mono and bis adducts, [Ru(NO)Cl3(dpaH)] = (2) and [Ru(NO)Cl(dpaH) 2]Cl2 = (3). The dpaH ligands coordinate cis to the Ru(NO) axis.The mono derivative is a model for a potential DNA groove‐spanning binuclear complex
{(tpada)} = (4) which has two DNA‐coordinating RuII centers, photo‐labile {Ru(NO)} 6 sites, and a groove‐spanning tether moiety.The binuclear assembly is prepared from the tethered dipyridylamine ligand N,N,N′,N′‐tetrakis(2‐pyridylmethyl)adipamide (tpada) which has recently been shown to provide a binuclear carrier complex suited to transporting RuII and PdII agents. A related complex, [Ru(NO)Cl(pida)] = (5) with the {Ru(NO)} 6 moiety bound to (2‐pyridylmethyl) iminodiacetate (pida2-) is also characterized as a potential “caged NO” carrier. Structural information concerning the
placement of the pyridyl donor groups relative to the {Ru(NO)} 6 unit has been obtained from  1H and  13C NMR and infrared methods, noting that a pyridyl donor trans to NO+ causes “trans strengthening” of this ligand for [Ru(NO)Cl(pida)], whereas placement of pyridyl groups cis to NO+ causes a weakening of the N‐O bond and a lower NO stretching frequency in the dpa‐based complexes.
Synthesis, Characterization, In Vitro and In Vivo Screening of Unsymmetrical Borole Complexes of 2‐Hydroxy‐N‐Phenylbenzamide and its Derivatives
Authors: Pandey Taruna , Singh R. V.
Published: March 2007

Biochemical aspects, synthesis and characterization of some boron complexes of 2‐hydroxy‐N‐phenylbenzamide (HOPhBenz) and its semicarbazone (HOPhBenz.SCZH) and thiosemicarbazone (HOPhBenz.TSCZH) are described. These derivatives were prepared by the reactions of 2‐isopropoxy‐4‐methyl‐1,3,2‐dioxaborolane, and 2‐isopropoxy‐4‐methyl‐1,3,2‐dioxaborinane with 2‐hydroxy‐N‐phenylbenzamide, 1‐[(2‐hydroxyphenyl)‐1‐N‐phenylamino]hydrazinecarboxamide (HOPhBenz.SCZH), and 1‐[(2‐hydroxyphenyl)‐1‐N‐phenylamino]hydrazinecarbothioamide(HOPhBenz.TSCZH) in a 1:1 molar ratio. In order to assess the increase of the inhibitor potency, (HOPhBenz), (HOPhBenz.SCZH), (HOPhBenz.TSCZH) and their boron complexes have been tested in vitro against a number of pathogenic fungi and bacteria at different concentrations and were found to possess remarkable fungicidal and bactericidal properties. The testicular sperm density, testicular sperm morphology, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trials and biochemical parameters of reproductive organs are discussed.
Development of Acid‐Sensitive Platinum(II) Complexes With Protein‐Binding Properties
Authors: Schütte M. T. , Mülhaupt R. , Kratz F.
Published: March 2007

Four new protein‐binding platinum(II) complexes, 10, 11, 21, 22, in which the dichloroplatinum moiety is coordinated either to a carbon‐substituted or a nitrogen‐substituted ethylene diamino ligand, were prepared in ten‐step syntheses. According to pH‐dependent stability studies with strictly related compounds, 11 and 22 exhibit acid‐sensitive properties.
On the Publication of the Results of X‐Ray Crystal Structure Analysis in Metal-Based Drugs
Authors: Tiekink Edward R. T.
Published: March 2007

While it would be normal to mention that a crystal structure determination is reported, it
is not necessary to include crystallographic data in the Abstract.
Evaluation of Antibacterial Properties of Triorganotin Carboxylates Containing Functionalised Ester Groups in Tests Against Some Pathogenic Bacteria
Authors: Koshy J. , Ansary A. , Lo K. M. , Das V. G. Kumar
Published: March 2007

Bacterial screening employing the agar diffusion test on triphenyltin carboxylates containing various
functional residues in the ester moiety revealed appreciable differences in their activities relative to
triphenyltin acetate. Among these, [3‐(Diethylphosphono)propionato] triphenyltin (1) and [N‐cyclohexylcarbamoyl) glycinato] triphenyltin displayed activities comparable to tri‐n‐butyltin cinnamate (2) towards both Gram‐positive and Gram‐negative bacteria; the latter compound was the most active among the eleven triorganotin compounds tested, which included cyclopentyldiphenyltin hydroxide (3) and its methacrylate derivative. Applying the more quantitative plate count and optical density tests on compounds 1-3, it was shown that their inhibitory activity ranked in the order 2 > 3 >1. Significantly, 3 caused around 90% inhibition of both Eschechia coli (−) and Pseudomonas aeruginosa (−) when incubated for 24 h at 37±1℃
at the 10.0 μg/ mL concentration level. Compound 2 was less effective against P.aeruginosa than against E.coli. While the Gram‐positive bacteria were all readily inhibited, Bacillus subtilis (+) appeared to the most susceptible among them towards the test compounds.
Construction of Ru(II) Polypyridyl Based Macrocycles: Synthesis, Characterization, Electrochemical, Li+ Binding, Antitumour and Anti‐HIV properties
Authors: Mishra Lallan , Sinha Ragini , Pandey P. C.
Published: March 2007

Some ruthenium (II) polypyridyl complexes with a bis‐chalcone (obtained by the condensation of 3‐methyl‐thiophene‐2‐carboxaldehyde and 4‐acetyl pyridine) have been synthesized and characterized
spectroscopically (IR, NMR, UV/Vis), conductimetric, elemental analysis and FAB mass data. Their
luminescent, redox and Li+ binding properties have been studied. The anti‐HIV and antitumour activities
have also been reported.
Activity of Pt(II) and Ru(III) Triazolopyrimidine Complexes Against Parasites of the Genus Leishmania, Trypanosomas and Phytomonas
Authors: Salas Juan M. , Quirós Miguel , Abul Haj Mohammad , Magán Rosa , Marín Clotilde , Sáchez-Moreno Manuel , Faure René
Published: March 2007

The synthesis and characterization of two Pt(II) Complexes with the isomeric ligands 4,5‐dihydro‐5‐oxo‐
[1,2,4]triazolo‐[ 1,5‐a]pyrimidine (5HtpO) and 4,7‐dihydro‐7‐oxo‐[ 1,2,4]‐triazolo‐[ 1,5‐a]pyrimidine (7HtpO) are
described, as well as a Ru(III) complex with 7HtpO. The crystal structure of cis‐[PtCl2(7HtpO) 2].2H2O has been solved by X‐ray diffraction analysis. In vitro activity of the new isolated complexes against the epimastigote form of T. cruzi, procyclic form of T. b. brucei and promastigote form of L. donnovani and P. characias has
also been studied. The three complexes markedly affect the growth of the parasites and none of them shows
cytotoxicity against macrophage of the J774.2 line at the heaviest dosages used.