bluuebunny/crossref_metadata_2025_split huggingface dataset:
ChemInform Abstract: Dual Amine‐ and Broensted Acid‐Catalyzed α‐Allylic Alkylation of Aldehydes.
Authors: Xu Li‐Wen , Gao Guang , Gu Feng‐Lei , Sheng Hao , Li Li , Lai Guo‐Qiao , Jiang Jian‐Xiong 
Published: October 2010

AbstractA simple and palladium‐free, catalytic variant of title reaction is conducted under air without the need for dried solvents; water is the only side product of the reaction.
ChemInform Abstract: Michael Reaction of Nitroalkanes with β‐Nitroacrylates under a Solid Promoter: Advanced Regio‐ and Diastereoselective Synthesis of Nitro‐Functionalized α,β‐Unsaturated Esters and 1,3‐Butadiene‐2‐carboxylates.
Authors: Palmieri Alessandro , Gabrielli Serena , Ballini Roberto 
Published: October 2010

AbstractThe regio‐ and diastereoselective syntheses of several nitro‐functionalized α,β‐unsaturated esters such as (III) or (IX)/(X) and — at higher temperatures — butadienecarboxylates (IV)/(V) proceed under eco‐friendly conditions, using the eco‐compatible solvent ethyl acetate and a solid and reusable promoter.
ChemInform Abstract: Copper‐Catalyzed Coupling Reaction of C—OMe Bonds Adjacent to a Nitrogen Atom with Terminal Alkynes.
Authors: Yao Bangben , Zhang Yuhong , Li Yong 
Published: October 2010

AbstractCu‐catalyzed treatment of formamide acetals or the methoxy amine (IX) with terminal alkynes allows simple and efficient access to a wide range of 3‐amino‐1,4‐diynes.
ChemInform Abstract: Design, Synthesis, and Application of Chiral Electron‐Poor Guanidines as Hydrogen‐Bonding Catalysts for the Michael Reaction.
Authors: Thai Karen , Gravel Michel 
Published: October 2010

AbstractThe first example of chiral electron‐poor guanidine catalysis through hydrogen‐bonding interactions without prior protonation to form a guanidinium species is reported.
ChemInform Abstract: Chemoselective and Chemospecific Protection and Deprotection of a Carbonyl Group Using Polystyrene Divinylbenzene Sulfonic Acid.
Authors: Verma Sanjeev K. , Sathe Manisha , Kaushik M. P. 
Published: October 2010

AbstractThe chemoselective protection and deprotection of carbonyl groups using cross‐linked polystyrene divinylbenzene sulfonic acid as a heterogenous catalyst is demonstrated.
ChemInform Abstract: Silica‐Supported HgSO4/H2SO4: A Convenient Reagent for the Hydration of Alkynes under Mild Conditions.
Authors: Mello Rossella , Alcalde‐Aragones Ana , Gonzalez‐Nunez Maria Elena 
Published: October 2010

AbstractThe inexpensive reagent allows isolation of the products by simply filtering and evaporating the solvent.
ChemInform Abstract: Tandem Suzuki—Miyaura Cross‐Coupling/Dehydrobromination of 1,1‐Dibromoalkenes to Alkynes with a Cyclobutene‐1,2‐diylbis(imidazolium) Salt as Catalyst Precursor.
Authors: Rahimi Alireza , Schmidt Andreas 
Published: October 2010

AbstractDibromoalkenes, prepared from aldehydes under Corey—Fuchs conditions, undergo a tandem process in one pot to give the desired alkyne products within a short time.
ChemInform Abstract: Large‐Scale Preparation of Aromatic Fluorides via Electrophilic Fluorination with Functionalized Aryl‐ or Heteroarylmagnesium Reagents.
Authors: Yamada Shigeyuki , Knochel Paul 
Published: October 2010

AbstractGrignard reagents, prepared either by halogen—magnesium exchange or direct magnesium insertion in the presence of LiCl, are treated with N‐fluorobenzenesulfonamide to afford the corresponding aromatic fluorides.
ChemInform Abstract: Mesoporous Aluminosilicate Catalyzed Sakurai Allylation and Mukaiyama Aldol Reaction of Acetals.
Authors: Ito Suguru , Hayashi Akira , Komai Hirotomo , Kubota Yoshihiro , Asami Masatoshi 
Published: October 2010

AbstractAllyltrimethylsilane (II) and silyl enol ether (X) react with acetals and cyclohexanone dimethylketal in the presence of Al‐MCM‐41 under mild conditions to produce homoallyl ethers and β‐methoxy ketones, respectively.
ChemInform Abstract: Effective Cleavage of Ditertiary Glycols via Vanadium(V)‐Catalyzed Aerobic Oxidation.
Authors: Kirihara Masayuki , Yoshida Katsumi , Noguchi Takuya , Naito Sayuri , Matsumoto Nobuchika , Ema Yukinori , Torii Motoya , Ishizuka Yuki , Souta Ikuo 
Published: October 2010

AbstractThe optimized conditions allow a clean oxidative cleavage in the case of (relatively) simple glycol substrates.
ChemInform Abstract: A New and Efficient Aerobic Oxidation of Aldehydes to Carboxylic Acids with Singlet Oxygen in the Presence of Porphyrin Sensitizers and Visible Light.
Authors: Hajimohammadi Mahdi , Safari Nasser , Mofakham Hamid , Shaabani Ahmad 
Published: October 2010

AbstractThe reaction is tested in the presence of different tetraaryl porphyrins and analogous Zn complexes and TMP is found to be the most effective promoter.
ChemInform Abstract: PdII‐Catalyzed Oxidative 1,1‐Diarylation of Terminal Olefins.
Authors: Werner Erik W. , Urkalan Kaveri B. , Sigman Matthew S. 
Published: October 2010

AbstractThe reaction is tolerant to a variety of functionalities and proceeds with complete retention of the optical purity, when a chiral substrate is applied [cf.
ChemInform Abstract: Triazole‐Functionalized N‐Heterocyclic Carbene Complexes of Palladium and Platinum and Efficient Aqueous Suzuki—Miyaura Coupling Reaction.
Authors: Gu Shaojin , Xu Hui , Zhang Na , Chen Wanzhi 
Published: October 2010

AbstractA series of N‐heterocyclic carbene platinum or palladium complexes are synthesized using the click chemistry.
ChemInform Abstract: Synthesis of Functionalized Bisarylacetylene Derivatives from Acetylene Gas over Nanosized Carbon Ball Supported Palladium Catalyst.
Authors: Yum Eul Kgun , Son Jong Woo , Kim Soo Kwang , Kim Sung Nam , Kim Kyung Mahn , Lee Chul Wee 
Published: October 2010

AbstractA variety of the title compounds (III) is obtained under mild reaction conditions.
ChemInform Abstract: Microwave‐Assisted Regioselective Synthesis of trans‐1‐Arenesulfonyl‐2‐ethoxycarbonyl‐3‐phenylazetidines.
Authors: Malik Sarika , Nadir Upender K. , Pandey Pramod S. 
Published: October 2010

AbstractThe ring expansion reaction of aziridines (I) and (V), respectively by ylides (II) is studied.
ChemInform Abstract: Gold Catalysis: Desymmetrization in the Furan—Yne Reaction.
Authors: Hashmi A. Stephen K. , Woelfle Michael , Ata Filiz , Frey Wolfgang , Rominger Frank 
Published: October 2010

AbstractThe reaction of diketones (I) with Grignard reagent (II) affords a mixture of anti‐ and syn‐homoproparyglic diols.
ChemInform Abstract: Directed Lithiation of N‐Benzenesulfonyl‐3‐bromopyrrole. Electrophile‐Controlled Regioselective Functionalization via Dynamic Equilibrium Between C‐2 and C‐5 Lithio Species.
Authors: Fukuda Tsutomu , Ohta Takeshi , Sudo Ei‐ichi , Iwao Masatomo 
Published: October 2010

AbstractThe formation of the 2‐ or 5‐substituted pyrroles is determined by a nature of the electrophiles used and in some cases the temperature.
ChemInform Abstract: Synthesis of cis‐3,4‐Diaryl α‐Methylene‐γ‐butyrolactams via Sonochemical Barbier‐Type Reaction.
Authors: Lee Adam Shih‐Yuan , Chang Yu‐Ting 
Published: October 2010

AbstractThe process is optimal if N‐tosylimines are used to give the title compounds selectively in moderate to good yields.
ChemInform Abstract: Asymmetric Quadruple Aminocatalytic Domino Reactions to Fused Carbocycles Incorporating a Spirooxindole Motif.
Authors: Jiang Kun , Jia Zhi‐Jun , Yin Xiang , Wu Li , Chen Ying‐Chun 
Published: October 2010

AbstractA three‐component, domino Michael—Michael—Michael—aldol process of the indole‐derived substrates of the type (I) with two identical or different molecules of α,β‐unsaturated aldehydes under quadruple iminium/enamine/iminium/enamine catalysis affords a variety of the enantiomerically pure hydroindane derivatives, bearing six contiguous stereocenters and a spirooxindole motif with complete diastereoselectivities [cf.
ChemInform Abstract: Efficient Carbonate Synthesis under Mild Conditions Through Cycloaddition of Carbon Dioxide to Oxiranes Using a Zn(salphen) Catalyst.
Authors: Decortes Antonello , Martinez Belmonte Marta , Benet‐Buchholz Jordi , Kleij Arjan W. 
Published: October 2010

AbstractMonosubstituted oxiranes are suitable substrates for the process.
ChemInform Abstract: Catalytic Asymmetric 6π‐Electrocyclization: Accessing Highly Substituted Optically Active 2‐Pyrazolines via Diastereoselective Alkylations.
Authors: Mueller Steffen , List Benjamin 
Published: October 2010

AbstractThe chiral phosphinic acid BPN catalyzes the 6π‐electrocyclization of hydrazones to give 2‐pyrazolines in high yield and generally good to excellent e.e.
ChemInform Abstract: Synthesis of 1,3‐Diaryl‐Substituted Indazoles Utilizing a Suzuki Cross‐Coupling/Deprotection/N‐Arylation Sequence.
Authors: Salovich James M. , Lindsley Craig W. , Hopkins Corey R. 
Published: October 2010

AbstractSubstrate (I) is highly suitable for the title sequence which affords a broad spectrum of target compounds.
ChemInform Abstract: Room Temperature Synthesis of Tri‐, Tetrasubstituted Imidazoles and Bis‐Analogues by Mercaptopropylsilica (MPS) in Aqueous Methanol: Application to the Synthesis of the Drug Trifenagrel.
Authors: Mukhopadhyay Chhanda , Tapaswi Pradip Kumar , Drew Michael G. B. 
Published: October 2010

AbstractA modified procedure for the preparation of mercaptopropylsilica is developed and the catalyst is efficiently used for the synthesis of various title compounds including the novel potent platelet aggregation inhibitor trifenagrel (IIIb).
ChemInform Abstract: A Convenient and Efficient Synthesis of C‐Carbamoyl‐1,2,3‐triazoles from Alkyl Bromide by a One‐Pot Sequential Addition: Conversion of Ester to Amide Using Zr(Ot‐Bu)4.
Authors: Yang Dongsik , Kwon Mihyun , Jang Yujin , Jeon Heung Bae 
Published: October 2010

AbstractThe microwave‐assisted one‐pot three‐step procedure involves in situ generation of alkyl azides,1,3‐dipolar cycloaddition with ester (I) and amide formation.
ChemInform Abstract: New Functionalized Aminofurazans as Potential Antimitotic Agents in the Sea Urchin Embryo Assay.
Authors: Sheremetev Aleksei B. , Dmitriev Dmitrii E. , Lagutina Nataliya K. , Raihstat Mikhail M. , Kiselyov Alex S. , Semenova Marina N. , Ikizalp Natalie N. , Semenov Victor V. 
Published: October 2010

AbstractA variety of new aminofurazans is designed, synthesized and evaluated for their antimitotic activity using a sea urchin embryo assay.
ChemInform Abstract: A Novel Synthesis of 1,5‐Disubstituted Fluorinated Tetrazoles from 1,1‐Difluoroazides.
Authors: Polivanova Anna G. , Shkavrov Sergey V. , Churakov Andrei V. , Lermontov Anatoly S. , Lermontov Sergey A. 
Published: October 2010

AbstractThe reaction of difluoroazides with primary amines provides an excellent access to tetrazole products.
ChemInform Abstract: One‐Pot Synthesis of 2‐Amino‐4H‐chromen‐4‐yl Phosphonate Derivatives Using β‐Cyclodextrin as Reusable Catalyst in Water.
Authors: Murthy S. Narayana , Madhav B. , Reddy V. Prakash , Nageswar Y. V. D. 
Published: October 2010

AbstractA simple and efficient protocol is developed for the synthesis of title compounds bearing a phosphonate group as biostere of the ester moiety.
ChemInform Abstract: Imidazolium‐Based Phosphinite Ionic Liquid (IL‐OPPh2) as Reusable Catalyst and Solvent for the Knoevenagel Condensation Reaction.
Authors: Valizadeh Hassan , Gholipour Hamid 
Published: October 2010

AbstractA new method for the synthesis of (E)‐acrylates/benzylidenemalononitriles (III) and coumarins (VI) via Knoevenagel condensation of appropriate benz‐ or salicylaldehydes with active methylene compounds is described.
ChemInform Abstract: Selective One‐Pot Multicomponent Synthesis and anti‐Tubercular Evaluation of 5‐(Aryl/cyclohexylsulfanyl)‐2‐alkoxy‐4,6‐diarylnicotinonitriles.
Authors: Manikannan Ramaiyan , Muthusubramanian Shanmugam , Yogeeswari Perumal , Sriram Dharmarajan 
Published: October 2010

AbstractThirty highly substituted pyridine derivatives of type (V) are prepared in a four‐component one‐pot reaction and evaluated for their antitubercular activities.
ChemInform Abstract: One‐Pot Palladium‐Catalyzed Synthesis of Selectively Substituted Phenanthridines by Sequential Aryl—Aryl and Heck Couplings, Aza‐Michael and Retro‐Mannich Reactions.
Authors: Della Ca Nicola , Motti Elena , Mega Antonio , Catellani Marta 
Published: October 2010

AbstractIn spite of many steps involved, the title reaction is very simple and allows the synthesis of phenanthridines such as (IV) or (VII) using a one‐pot protocol.
ChemInform Abstract: New Method for the Anellation of a Pyridine Ring on Derivatives of Imidazole and Benzimidazole.
Authors: Potikha L. M. , Turelyk A. R. , Kovtunenko V. A. , Turov A. V. 
Published: October 2010

AbstractA simple method for the anellation of pyridine rings on imidazole or benzimidazole structures via base‐induced intramolecular cyclization reactions of quaternary (2,4‐diaryl‐4‐oxo‐2‐butenyl)imidazolium salts (I) is given.
ChemInform Abstract: Polycyclic N‐Heterocyclic Compounds. Part 65. Ring Cleavage Reactions of Fused Furo[2,3‐c]isoquinolines and Related Compounds with Various Nucleophiles.
Authors: Okuda Kensuke , Deguchi Hiroshi , Hirota Takashi , Sasaki Kenji 
Published: October 2010

AbstractReaction of fused 2,3‐dihydrofuro[2,3‐b]pyridines with various nucleophiles gives dihydrofuran ring cleaved products.
ChemInform Abstract: One‐Pot Synthesis of Benzo[a]phenanthrin‐5‐ones by Photoinduced Cycloaddition of 3‐Chloroisoquinolin‐1‐ones with Styrenes.
Authors: Li Bing , Han Bing , Shi Zong‐jun , Ren Yu‐wei , Lu Shen‐ci , Zhang Wei 
Published: October 2010

AbstractPhotoreactions of substrates (I) and (IV) with styrenes offers a short route to the target compounds via a photoinduced dechlorinative annulation.
ChemInform Abstract: Facile and Efficient One‐Pot Synthesis of β‐Carbolines.
Authors: Tang Jian‐Guo , Liu Han , Zhou Zhong‐Yu , Liu Ji‐Kai 
Published: October 2010

Abstractusing the Pictet—Spengler reaction of tryptophan ester (I) with aldehydes (II) followed by aromatization using cyanuric chloride
ChemInform Abstract: A Simple and Efficient Approach to the Synthesis of 2‐Phenylquinazolines via sp3 C—H Functionalization.
Authors: Zhang Jintang , Zhu Dapeng , Yu Chenmin , Wan Changfeng , Wang Zhiyong 
Published: October 2010

AbstractA wide range of bis‐, tri‐ and tetrasubstituted quinazolines is prepared in mostly good yields.
ChemInform Abstract: Novel Approach for the Synthesis of Five‐Membered‐Ring‐Fused Pyrazinones.
Authors: Gembus Vincent , Janvier Solenn , Lecouve Jean‐Pierre , Gloanec Philippe , Marsais Francis , Levacher Vincent 
Published: October 2010

AbstractA new route to access important pharmaceutical intermediates for the synthesis of constrained fused pyrazinones is developed.
ChemInform Abstract: Investigations in the Field of Benzoxazines. Part 15. Tandem Heterocyclizations with the Participion of 2‐Formylbenzoic Acid. The Synthesis of Isoindolo[1,2‐b][1,3]‐ and ‐[2,1‐a][3,1]benzoxazinones.
Authors: Gromachevskaya E. V. , Pilipenko A. S. , Butin A. V. , Zavodnik V. E. , Krapivin G. D. 
Published: October 2010

AbstractTitle compounds (III) and (VI) are conveniently synthesized by heterocyclization reaction of 2‐formylbenzoic acids with binucleophiles (I) or (IV), respectively.
ChemInform Abstract: Synthesis of Schaefferals A (VIIIa) and B (VIIIb), Unusual Phenylhydrazine Derivatives from Mushrooms of the Genus Agaricus.
Authors: Kileci‐Ksoll Rengin , Winklhofer Christian , Steglich Wolfgang 
Published: October 2010

AbstractThe structures are unambiguously confirmed by a convenient five‐step total synthesis.
ChemInform Abstract: Four New ent‐Kaurane Diterpenoids from the Fruits of Annona cherimola.
Authors: Miyashita Hiroyuki , Nishida Makiko , Okawa Masafumi , Nohara Toshihiro , Yoshimitsu Hitoshi 
Published: October 2010

AbstractTitle substances (I) and (II) as well as eight known diterpenoids are found in A.
ChemInform Abstract: Total Synthesis of (.+‐.)‐Elegansidiol, (.+‐.)‐Farnesiferol B, and (.+‐.)‐Farnesiferol D.
Authors: Yadav Jhillu Singh , Satyanarayana Kamani , Sreedhar Pamu , Srihari Pabbaraja , Shaik Thokhir Basha , Kalivendi Shasi Vardhan 
Published: October 2010

AbstractElegansidiol (Ia), farnesiferol B (Ib), and farnesiferol D (II) are screened for their effects on growth inhibition and cytotoxicity in two human cancer cell lines.
ChemInform Abstract: Versatile Synthesis of New Cytotoxic Agents Structurally Related to Hemiasterlins.
Authors: Simoni Daniele , Lee Ray M. , Durrant David E. , Chi Nai‐Wen , Baruchello Riccardo , Rondanin Riccardo , Rullo Cinzia , Marchetti Paolo 
Published: October 2010

AbstractA series of structural analogues of the antimitotic tripeptides hemiasterlins is synthesized by a flexible approach using α‐bromoacid, e.g. (I), as starting material and an Ag2O‐promoted nucleophilic substitution as the key step Variation of (I), which is available from any diazotizable α‐amino acid and of the nucleophiles allows the generation of hemiasterlin libraries.
ChemInform Abstract: Total Synthesis and Assignment of the Side Chain Stereochemistry of LI‐F04a: An Antimicrobial Cyclic Depsipeptide.
Authors: Cochrane James R. , McErlean Christopher S. P. , Jolliffe Katrina A. 
Published: October 2010

AbstractPreparation of both side‐chain epimers as well as spectral investigations establish the configuration at C‐3 of the natural substance as (R).
ChemInform Abstract: Concise Synthesis of Five‐Membered Ring Carbasugars Based on Key Ring‐Closing Metathesis.
Authors: Yang Ya‐Xi , Li Zheng , Feng Hui‐Jin , Chen Guo‐Rong , Li Yuan‐Chao 
Published: October 2010

AbstractReadily available (R)‐2,3‐O‐isopropylidene glyceraldehyde is used as starting material for the preparation of chiral dienes (I), (III), and (V) which undergo ring‐closing metathesis to produce five‐membered ring carbasugars.
ChemInform Abstract: Penicinoline, a New Pyrrolyl 4‐Quinolinone Alkaloid with an Unprecedented Ring System from an Endophytic fungus Penicilium sp.
Authors: Shao Chang‐Lun , Wang Chang‐Yun , Gu Yu‐Cheng , Wei Mei‐Yan , Pan Jia‐Hui , Deng Dong‐Sheng , She Zhi‐Gang , Lin Yong‐Cheng 
Published: October 2010

AbstractThe new alkaloid penicinoline (I) is isolated from a mangrove endophytic fungus.
ChemInform Abstract: Antitrypanosomal Alkaloids from Polyalthia suaveolens (Annonaceae): Their Effects on Three Selected Glycolytic Enzymes of Trypanosoma brucei.
Authors: Ngantchou Igor , Nyasse Barthelemy , Denier Colette , Blonski Casimir , Hannaert Veronique , Schneider Bernd 
Published: October 2010

AbstractThe phytochemical study of stem barks of P.
ChemInform Abstract: New Pyrrolidine Alkaloids from the Roots of Pandanus amaryllifolius.
Authors: Tan Mario A. , Kitajima Mariko , Kogure Noriyuki , Nonato Maribel G. , Takayama Hiromitsu 
Published: October 2010

AbstractPandamarilactonine‐E (I), ‐F (II) (and its N‐oxide) and ‐G (III) are identified.
ChemInform Abstract: Untenolide A, a New Polyketide from an Okinawan Marine Sponge Plakortis sp.
Authors: Ishiguro Yuichiro , Kubota Takaaki , Fromont Jane , Shiro Motoo , Kobayashi Jun'ichi 
Published: October 2010

AbstractPreliminary studies do not reveal any cytotoxic effects.
ChemInform Abstract: New Rancinamycin Analogues from Streptomyces lincolnensis.
Authors: Kim Mi Ae , Kim Eun La , Kim Kyoung‐Ja , Hong Jongki , Bao Baoquan , Jung Jee H. 
Published: October 2010

AbstractLincitol A (Ia) and B (Ib) and the benzaldehyde derivative (II) are isolated from Streptomyces lincolnensis.
ChemInform Abstract: New Estrogenic Compounds Isolated from Broussonetia kazinoki.
Authors: Lee Da Yeon , Kim Do Hee , Lee Hwa Jin , Lee YoungJoo , Ryu Kwang Hee , Jung Bo‐In , Song Yun Seon , Ryu Jae‐Ha 
Published: October 2010

AbstractKazinol U (I) and kazinol I (II) are isolated from the title plant as new isoprenylated flavans together with the known compounds broussonin A and tupichinol C.
ChemInform Abstract: Metabolites from the Mangrove Endophytic Fungus Phomopsis sp. (#zsu‐H76).
Authors: Yang Jianxiang , Xu Fang , Huang Caihuan , Li Jing , She Zhigang , Pei Zhong , Lin Yongcheng 
Published: October 2010

AbstractPrimary bioassays show that (I) accelerates the growth of subintestinal vessel plexus (SIV) branch markedly, whereas (IIb) shows inhibition of SIV.
ChemInform Abstract: Rational Design and Synthesis of 4‐O‐Substituted Phenylmethylenethiosemicarbazones as Novel Tyrosinase Inhibitors.
Authors: Yi Wei , Cao Rihui , Chen Zhiyong , Yu Liang , Wen Huan , Yan Qin , Ma Lin , Song Huacan 
Published: October 2010

AbstractA series of thiosemicarbazones is designed, synthesized, and evaluated as mushroom tyrosinase inhibitor.
Synthesis, Cytotoxicity, and COMPARE Analysis of Ferrocene and [3]Ferrocenophane Tetrasubstituted Olefin Derivatives against Human Cancer Cells
Authors: Görmen Meral , Pigeon Pascal , Top Siden , Hillard Elizabeth A. , Huché Michel , Hartinger Christian G. , de Montigny Frédéric , Plamont Marie‐Aude , Vessières Anne , Jaouen Gérard 
Published: October 2010

AbstractHerein we report the antiproliferative effects of a series of 28 compounds against the MDA‐MB‐231 breast cancer cell line, including the synthesis of seven new [3]ferrocenophanyl and four new ferrocenyl compounds. For each p‐R‐phenyl substitution pattern investigated, the [3]ferrocenophanyl derivatives were more cytotoxic than the corresponding ferrocenyl derivative, with the highest activity found for compounds with protic substituents. Theoretical calculations of the HOMO–LUMO gap for the molecules in the Fe3+ oxidation state suggest a higher reactivity for the [3]ferrocenophanyl derivatives. A lead compound from each series, a [3]ferrocenophanyl and a ferrocenyl compound, possessing two phenol groups, were screened against the NCI/DTP 60‐cell‐line panel. The mean activity over all cell lines was better than cisplatin for both compounds, and both compounds showed subpanel selectivity for leukemia, CNS cancer, and renal cancer. Low systemic toxicity and lack of interaction with DNA (when in the reduced form), suggest that the compounds may act as prodrugs.
Dynamic changes in 1H‐MR relaxometric properties of cell‐internalized paramagnetic liposomes, as studied over a five‐day period
Authors: Kok Maarten B. , Strijkers Gustav J. , Nicolay Klaas 
Published: October 2010

AbstractMolecular imaging based on MRI requires the use of amplification strategies in order to achieve sufficient sensitivity for the detection of low‐level molecular markers. Recently, we described a combination of two amplification methods: (i) the use of paramagnetic liposomes that can be prepared with a high payload of Gd3+‐containing lipid; and (ii) targeting to a cell‐surface receptor that can undergo multiple rounds of nanoparticle delivery in the cell, followed by recycling to the cell membrane. Liposome uptake was monitored over a period of 24 h and was found to lead to massive delivery in subcellular compartments. The present study aimed to monitor the longer‐term fate of the cell‐internalized contrast material by studying its relaxometric properties over 5 days, following an initial 24 h loading period. Circa 25% of the Gd3+‐content delivered to the cells via integrin‐targeted liposomes was lost in the first 24 h, which led to 65 and 77% reductions in R1 and R2, respectively, as compared with the original R1 and R2 enhancements. This implies that the remaining cell‐associated gadolinium had relatively low effective r1 and r2 relaxivities. It is proposed that this is due to gradual release of Gd3+ from the chelate in the cell, followed by sequestration in an MR silent state. Most of the gadolinium internalized by cells following incubation with non‐targeted liposomes was released in the 5‐day follow‐up period. Copyright © 2010 John Wiley & Sons, Ltd.