bluuebunny/crossref_metadata_2025_split huggingface dataset:
Mutagenesis of Key Residues in the Binding Center of l‐Aspartate‐β‐Semialdehyde Dehydrogenase from Escherichia coli Enhances Utilization of the Cofactor NAD(H)
Authors: Xu Xiaoshu , Chen Jun , Wang Qingzhuo , Duan Chunlan , Li Yan , Wang Renxiao , Yang Sheng 
Published: December 2015

Abstractl‐Aspartate‐β‐semialdehyde dehydrogenase (ASADH) is a key enzyme in the aspartate pathway. In bacteria, ASADH is highly specific for the cofactor NADP+ rather than NAD+. Limited information on cofactor utilization is available, and neither the wild‐type protein nor the available mutants could utilize NAD+ efficiently. In this study, we identified several residues crucial for cofactor utilization by Escherichia coli ASADH (ecASADH) by mutating residues within the cofactor binding center. Among the investigated mutants, ecASADH‐Q350N and ecASADH‐Q350N/H171A, which exhibited markedly improved NAD+ utilization, were further investigated by various biochemical approaches and molecular modeling. Relative to the wild type, the two mutants showed approximately 44‐fold and 66‐fold increases, respectively, in the constant kcat/Km of NAD+. As desired, they could also utilize NADH efficiently to synthesize l‐homoserine in cascade reactions in vitro.
Electronically Strongly Coupled Divinylheterocyclic‐Bridged Diruthenium Complexes
Authors: Pfaff Ulrike , Hildebrandt Alexander , Korb Marcus , Oßwald Steffen , Linseis Michael , Schreiter Katja , Spange Stefan , Winter Rainer F. , Lang Heinrich 
Published: December 2015

AbstractComplexes [{Ru(CO)Cl(PiPr3)2}2(μ‐2,5‐(CHCH)2‐cC4H2E] (E=NR; R=C6H4‐4‐NMe2 (10 a), C6H4‐4‐OMe (10 b), C6H4‐4‐Me (10 c), C6H5 (10 d), C6H4‐4‐CO2Et (10 e), C6H4‐4‐NO2 (10 f), C6H3‐3,5‐(CF3)2 (10 g), CH3 (11); E=O (12), S (13)) are discussed. The solid state structures of four alkynes and two complexes are reported. (Spectro)electrochemical studies show a moderate influence of the nature of the heteroatom and the electron‐donating or ‐withdrawing substituents R in 10 a–g on the electrochemical and spectroscopic properties. The CVs display two consecutive one‐electron redox events with ΔE°′=350–495 mV. A linear relationship between ΔE°′ and the σp Hammett constant for 10 a–f was found. IR, UV/Vis/NIR and EPR studies for 10+–13+ confirm full charge delocalization over the {Ru}CHCH‐heterocycle‐CHCH{Ru} backbone, classifying them as Class III systems according to the Robin and Day classification. DFT‐optimized structures of the neutral complexes agree well with the experimental ones and provide insight into the structural consequences of stepwise oxidations.
Enantioselective Total Synthesis of (+)‐Steenkrotin A and Determination of Its Absolute Configuration
Authors: Pan Saiyong , Gao Beiling , Hu Jialei , Xuan Jun , Xie Hujun , Ding Hanfeng 
Published: December 2015

AbstractThe first enantioselective total synthesis of (+)‐steenkrotin A has been achieved in 18 steps and 4.2 % overall yield. The key features of the strategy entail a Rh‐catalyzed O−H bond insertion followed by an intramolecular carbonyl‐ene reaction, two sequential SmI2‐mediated Ueno–Stork and ketyl–olefin cyclizations, and a cascade intramolecular aldol condensation/vinylogous retro‐aldol/aldol process with inversion of the relative configuration at the C7 position. The absolute configuration of (+)‐steenkrotin A was determined based on the stepwise construction of the stereocenters during the total synthesis.
Stereoselective Synthesis of the Proposed C79–C104 Fragment of Symbiodinolide
Authors: Takamura Hiroyoshi , Fujiwara Takayuki , Kawakubo Yohei , Kadota Isao , Uemura Daisuke 
Published: December 2015

AbstractStereoselective and streamlined synthesis of the proposed C79–C104 fragment 2 of symbiodinolide (1), a polyol marine natural product with a molecular weight of 2860, was achieved. In the synthetic route, the proposed C79–C104 fragment 2 was synthesized by utilizing a Julia–Kocienski olefination and subsequent Sharpless asymmetric dihydroxylation as key transformations in a convergent manner. Detailed comparison of the 13C NMR chemical shifts between the natural product and the synthetic C79–C104 fragment 2 revealed that the stereostructure at the C91–C99 carbon chain moiety of symbiodinolide (1) should be reinvestigated.
ChemInform Abstract: Synthesis and Thermoelectric Properties of N‐Type Half‐Heusler Compound VCoSb with Valence Electron Count of 19.
Authors: Zhang Hao , Wang Yumei , Huang Lihong , Chen Shuo , Dahal Heshab , Wang Dezhi , Ren Zhifeng 
Published: December 2015

AbstractVCoSb is prepared by arc melting of stoichiometric amounts of the elements to form ingots which then are ball milled to produce a nanostructured powder and finally hot pressed to form the bulk material.
ChemInform Abstract: Y‐Doped Li8ZrO6: A Li‐Ion Battery Cathode Material with High Capacity.
Authors: Huang Shuping , Wilson Benjamin E. , Wang Bo , Fang Yuan , Buffington Keegan , Stein Andreas , Truhlar Donald G. 
Published: December 2015

AbstractThe energetics, structural changes, and charge flows during charging and discharging processes for pure and Y‐doped Li8ZrO6 high‐capacity cathode materials are investigated by XRD, XPS, UV/VIS spectroscopy, electrochemical measurements, and quantum mechanical DFT calculations.
ChemInform Abstract: Synthesis, Structure, and Electrochemical Performance of High Capacity Li2Cu0.5Ni0.5O2 Cathodes.
Authors: Ruther Rose E. , Zhou Hui , Dhital Chetan , Saravanan Kuppan , Kercher Andrew K. , Chen Guoying , Huq Ashfia , Delnick Frank M. , Nanda Jagjit 
Published: December 2015

AbstractThe title compound is prepared by coprecipitation from aqueous solutions of Cu(NO3)2, Ni(NO3)2, NH4OH, and LiOH (50 °C, 3 h).
ChemInform Abstract: An All‐Metal Aromatic Sandwich Complex [Sb3Au3Sb3]3‐.
Authors: Pan Fu‐Xing , Li Lei‐Jiao , Wang Ying‐Jin , Guo Jin‐Chang , Zhai Hua‐Jin , Xu Li , Sun Zhong‐Ming 
Published: December 2015

AbstractDark red crystals of [K([2.2.2]cryptand)]3 [Sb3Au3Sb3] ·0.5PPh3·en (I) are prepared by addition of a toluene solution of Au(PPh3)Ph to a solution of K5Sb4 and [2.2.2]cryptand in en (25 °C, 4 h; 11% yield).
ChemInform Abstract: Catalyst‐Controlled Amino‐ versus Oxy‐Acetoxylation of Urea‐Tethered Alkenes: Efficient Synthesis of Cyclic Ureas and Isoureas.
Authors: Rao Wei‐Hao , Yin Xue‐Song , Shi Bing‐Feng 
Published: December 2015

AbstractThe regioselectivity of the acetoxycyclization of N‐allylureas to furnish either imidazoles or oxazoles is controlled by choice of the transition‐metal catalyst.
ChemInform Abstract: Copper‐Catalyzed Cross‐Coupling Reaction of Allyl Boron Ester with 1°/2°/3°‐Halogenated Alkanes.
Authors: Wang Guang‐Zu , Jiang Jian , Bu Xiao‐Song , Dai Jian‐Jun , Xu Jun , Fu Yao , Xu Hua‐Jian 
Published: December 2015

AbstractThe scalable method succeeds efficiently starting from primary, secondary, and tertiary alkyl bromides and tolerates various functional groups.
ChemInform Abstract: Enantioselective α‐Alkylation of Aldehydes by Photoredox Organocatalysis: Rapid Access to Pharmacophore Fragments from β‐Cyanoaldehydes.
Authors: Welin Eric R. , Warkentin Alexander A. , Conrad Jay C. , MacMillan David W. C. 
Published: December 2015

AbstractThe reaction of various aliphatic and aromatic aldehydes with α‐bromonitriles under either conditions A) or B) produces highly functionalized oxonitriles with excellent e.e.
ChemInform Abstract: Catalytic Enantioselective Peroxidation of α,β‐Unsaturated Aldehydes for the Asymmetric Synthesis of Biologically Important Chiral Endoperoxides.
Authors: Hu Lin , Lu Xiaojie , Deng Li 
Published: December 2015

AbstractThe method is utilized for the enantioselective construction of the core shared by all members of the stolonoxide family of anticancer natural products (VI).
ChemInform Abstract: Chemoselective Carbene Insertion into the N—H Bond over O—H Bond Using a Well‐Defined Single Site (P—P)Cu(I) Catalyst.
Authors: Ramakrishna Kankanala , Murali Mani , Sivasankar Chinnappan 
Published: December 2015

AbstractThe air‐stable catalyst renders possible the desired chemoselective insertion and avoids formation of olefinic products.
ChemInform Abstract: The Organocatalyzed Domino Michael—Aldol Reaction Revisited. Synthesis of Enantioenriched 3‐Hydroxycyclohexanone Derivatives by Reaction of Enals with α,α′‐Diaryl‐Substituted Acetone.
Authors: Guevara‐Pulido James O. , Andres Jose M. , Pedrosa Rafael 
Published: December 2015

AbstractContrary to previously described, it is shown that ketones with pKa <18 can be used as nucleophiles in the organocatalyzed Michael addition to α,β‐unsaturated aldehydes.
ChemInform Abstract: An Asymmetric Organocatalytic Quadruple Domino Reaction Employing a Vinylogous Friedel—Crafts/Michael/Michael/Aldol Condensation Sequence.
Authors: Philipps Arne R. , Fritze Lars , Erdmann Nico , Enders Dieter 
Published: December 2015

AbstractHighly functionalized cyclohexenecarbaldehydes bearing a 1,1‐bis[4‐(dialkylamino)phenyl]ethene moiety and three contiguous stereogenic centers are synthesized with very good diastereoselectivity, virtually complete enantiomeric excess, and good functional group tolerance.
ChemInform Abstract: Nickel‐Catalyzed Chemo‐, Regio‐ and Diastereoselective Bond Formation Through Proximal C—C Cleavage of Benzocyclobutenones.
Authors: Julia‐Hernandez Francisco , Ziadi Asraa , Nishimura Akira , Martin Ruben 
Published: December 2015

AbstractThe title reactions take place in the presence of various diene reactants as two‐carbon synthons under conditions A).
ChemInform Abstract: Palladium‐Catalyzed Intermolecular Oxyarylation of Vinylacetates with Retention of an Alkenyl Moiety.
Authors: Qiu Sheng‐Qi , Xu Yun‐He , Loh Teck‐Peng 
Published: December 2015

AbstractThe title method provides an efficient and simple method for preparation of multisubstituted vinyl esters.
ChemInform Abstract: Platinum‐Catalyzed Cascade Rearrangement Reaction of 1,5‐Diynyl Esters: Unusual Regioselective 1,5‐Hydride Migration.
Authors: Zhu Hui , Huang Jiapian , Fan Congbin , Chen Zhiyuan 
Published: December 2015

AbstractDiynes of type (I), (III), and (V) are found to undergo a PtCl2‐catalyzed highly regioselective 1,3‐acyloxy migration/pentannulation/1.5‐hydride shift process resulting in the formation of (E)‐2‐vinyl‐3‐oxo‐1‐methyleneindenes.
ChemInform Abstract: Stereoselective Synthesis of Activated 2‐Arylazetidines via Imino‐Aldol Reaction.
Authors: Ghorai Manas K. , Das Subhomoy , Das Kalpataru , Kumar Amit 
Published: December 2015

AbstractThe reaction of N‐sulfonyl imines [e.g. (I)] and esters [e.g. (II)] gives β‐amino esters [e.g. (III)], which are first reduced to alcohols [e.g. (IV)] and then cyclized to azetidines [e.g. (V)].
ChemInform Abstract: Alkylative Amination of Biogenic Furans Through Imine‐to‐Azaallyl Anion Umpolung.
Authors: Blume Fabian , Albeiruty Mhd. Haitham , Deska Jan 
Published: December 2015

AbstractA scalable, operationally simple transformation of N‐furfurylidene‐N‐(diphenylmethyl)amine, prepared from 1‐furfural and benzhydrylamine, with various alkyl halides to the corresponding furfurylamines is described.
ChemInform Abstract: RhIII‐Catalyzed [4 + 1] Annulations of 2‐Hydroxy‐ and 2‐Aminobenzaldehydes with Allenes: A Simple Method Toward 3‐Coumaranones and 3‐Indolinones.
Authors: Kuppusamy Ramajayam , Gandeepan Parthasarathy , Cheng Chien‐Hong 
Published: December 2015

AbstractThe title reaction renders possible an approach to various benzofuran and indoline structures with a series of functionalities at the aryl ring and an (E)‐configurated vinyl side chain at C‐2 of the heterocyclic part.
ChemInform Abstract: Synthesis, Rearrangement, and Hauser Annulation of 3‐Isocyanophthalides.
Authors: Mal Dipakranjan , Ghosh Ketaki , Chakraborty Soumen 
Published: December 2015

AbstractThe title compounds are obtained in two simple steps and can be rearranged to 3‐cyanoisobenzofuran‐1‐ones without the use of toxic cyanides.
ChemInform Abstract: Efficient Synthesis of 3‐Pyrrolin‐2‐one Derivatives in Aqueous Media.
Authors: Moshtaghi Zonouz Adeleh , Eskandari Issa , Notash Behrooz 
Published: December 2015

AbstractPyrrolinones are synthesized by a one‐pot, three‐component route at room temperature in water without the use of a catalyst or any additive.
ChemInform Abstract: Direct C—H Amination for Indole Synthesis from N‐Ts‐2‐Styrylaniline Derivatives Catalyzed by Copper Salt.
Authors: Chen Di , Mo Han‐Jie , Chen Ding‐Ben , Yang Jian‐Guo 
Published: December 2015

AbstractIndoles are synthesized in good yields by the direct intramolecular C—H amination reactions via copper catalyzed oxidation with potassium peroxodisulfate.
ChemInform Abstract: Cobalt(II)‐Catalyzed C(sp2)—H Alkynylation/Annulation with Terminal Alkynes: Selective Access to 3‐Methyleneisoindolin‐1‐one.
Authors: Zhang Lin‐Bao , Hao Xin‐Qi , Liu Zhan‐Jiang , Zheng Xin‐Xiang , Zhang Shou‐Kun , Niu Jun‐Long , Song Mao‐Ping 
Published: December 2015

AbstractThe cobalt(II)‐oxalate‐catalyzed reaction between arylacetylenes and N‐protected arylamides with pyridin N‐oxide as the directing group furnishes the title compounds in good to high yields and in a E/Z‐selective manner (Z).
ChemInform Abstract: Rhodium‐Catalyzed Enantioselective Hydroamination of Alkynes with Indolines.
Authors: Chen Qing‐An , Chen Zhiwei , Dong Vy M. 
Published: December 2015

AbstractBranched N‐allylic indolines are highly regio‐ and stereoselectively obtained by hydroamination of internal alkynes via tandem rhodium catalysis.
ChemInform Abstract: Copper‐Promoted Coupling of Carbon Dioxide and Propargylic Alcohols: Expansion of Substrate Scope and Trapping of Vinyl Copper Intermediate.
Authors: Ouyang Lu , Tang Xiaodong , He Haitao , Qi Chaorong , Xiong Wenfang , Ren Yanwei , Jiang Huanfeng 
Published: December 2015

AbstractIn the presence of N,N‐diisopropylethylamine, CuI efficiently catalyzes the coupling of internal propargylic alcohols with CO2 to afford the corresponding α‐alkylidene cyclic carbonates.
ChemInform Abstract: An Efficient Access to (1H‐Tetrazol‐5‐yl)furoxan Ammonium Salts via a Two‐Step Dehydration/[3 + 2]‐Cycloaddition Strategy.
Authors: Fershtat Leonid L. , Epishina Margarita A. , Kulikov Alexander S. , Ovchinnikov Igor V. , Ananyev Ivan V. , Makhova Nina N. 
Published: December 2015

AbstractTetrazolylfuroxans are sensitive to impact, friction, and electric discharge.
ChemInform Abstract: Highly Enantioselective Cascade Reaction Catalyzed by Squaramides: The Synthesis of CF3‐Containing Chromanes.
Authors: Wang Rui , et al.  
Published: December 2015

AbstractNitroalkenes bearing an additional ‐CF3 function react with 2‐hydroxychalcones in the presence of the cinchona alkaloid CASQ to produce the desired functionalized benzopyran structures in a completely stereoselective manner.
ChemInform Abstract: Enol‐Ugi Reaction of Hydroxycoumarins: Straightforward Synthesis of Amino Acid Derived Coumarin Enamines.
Authors: Neo Ana G. , Castellano Teresa G. , Marcos Carlos F. 
Published: December 2015

AbstractHydroxycoumarins bearing electron‐withdrawing groups are utilized as acidic components in Ugi‐type multicomponent‐condensations with various imines and isocyanides leading to 3‐ and 4‐coumarin enamines without the use of a catalyst.
ChemInform Abstract: Rh‐Catalyzed Sequential Oxidative C—H Activation/Annulation with Geminal‐Substituted Vinyl Acetates to Access Isoquinolines.
Authors: Chu Haoke , Sun Song , Yu Jin‐Tao , Cheng Jiang 
Published: December 2015

AbstractThe utility of this method is demonstrated in a short synthesis of papaverine (XVII).
ChemInform Abstract: Metal‐Free Radical [2 + 2 + 1] Carbocyclization of Benzene‐Linked 1,n‐Enynes: Dual C(sp3)—H Functionalization Adjacent to a Heteroatom.
Authors: Hu Ming , Fan Jian‐Hong , Liu Yu , Ouyang Xuan‐Hui , Song Ren‐Jie , Li Jin‐Heng 
Published: December 2015

AbstractThe title reaction leads to fused five‐membered carbocyclic hydrocarbons.
ChemInform Abstract: Palladium‐Catalyzed Double C—H Arylation Reaction: Tandem Synthesis of Benzo[a]imidazo[5,1,2‐cd]indolizines from Imidazo[1,2‐a]pyridines and o‐Dihaloarenes.
Authors: Wang Hanyang , Chen Chunxia , Huang Zhangjie , Yao Liping , Li Bin , Peng Jinsong 
Published: December 2015

AbstractThe title indolizines are obtained by highly regiocontrolled intermolecular C‐3 arylation of imidazopyridines and subsequent intramolecular C‐5 arylation.
ChemInform Abstract: Studies of Stereochemistry of 3‐(Arylhydrazono)furan‐2(3H)‐ones, Synthesis of 4‐(Arylhydrazono)pyridazin‐3(1H)‐ones.
Authors: Maiorova Oksana A. , Babkina Natalya V. , Egorova Alevtina Yu. 
Published: December 2015

AbstractPyridazine derivatives (IV) are synthesized via azocoupling of furanones of type (I) followed by hydrazinolysis of 3‐(arylhydrazono)furan‐2(3H)‐ones (III) which are proved to exist preferentially in the E‐hydroazone form.
ChemInform Abstract: Perchloric Acid‐Functionalized Silica Nanosphere as Novel and Green Catalyst for the Synthesis of 2H‐Indazolo[2,1‐b]phthalazinetrione Derivatives.
Authors: Chegeni Mahdieh , Khazaei Ardeshir , Rahmati Sadegh , Fekri Mohammad Hossein 
Published: December 2015

Abstractvia multicomponent reaction of phthalhydrazide (I) with dimedone and aldehydes under solvent‐free conditions (14 examples)
ChemInform Abstract: Microwave‐Assisted Synthesis of Novel Perimidinium Salts as N‐Heterocyclic Carbene Precursors: Involvement in Palladium‐Catalyzed Cross‐Coupling Reactions.
Authors: Onar Gulnihan , Karatas Mert Olgun , Alici Buelent , Cetinkaya Engin 
Published: December 2015

AbstractPerimidinium salts are synthesized and used as catalysts in Heck and Suzuki reactions affording styrenes or biaryl derivatives, resp., in good yields.
ChemInform Abstract: Gold‐Catalyzed Formal [4π + 2π]‐Cycloadditions of tert‐Butyl Propiolates with Aldehydes and Ketones to Form 4H‐1,3‐Dioxine Derivatives.
Authors: Karad Somnath Narayan , Chung Wei‐Kang , Liu Rai‐Shung 
Published: December 2015

AbstractAryl, hetaryl, alkenyl, and alkyl substituted tert‐butyl propiolates react with aryl, hetaryl, alkenyl, and alkyl aldehydes as well as cyclic and acyclic dialkyl and arylalkyl ketones to form 4H‐1,3‐dioxine derivatives in high yields.
ChemInform Abstract: Ruthenium‐ and Palladium‐Catalyzed Consecutive Coupling and Cyclization of Aromatic Sulfoximines with Phenylboronic Acids: An Efficient Route to Dibenzothiazines.
Authors: Chinnagolla Ravi Kiran , Vijeta Arjun , Jeganmohan Masilamani 
Published: December 2015

AbstractApplication of enantioenriched sulfoxime substrates allows for the preparation of enantiomerically pure dibenzothiazines.
ChemInform Abstract: An Expedient Route to Highly Diversified [1,2,3]Triazolo[1,5‐a][1,4]benzodiazepines and Their Evaluation for Antimicrobial, Antiproliferative and in silico Studies.
Authors: Sudhapriya N. , Nandakumar A. , Arun Y. , Perumal P. T. , Balachandran C. , Emi Nobuhiko 
Published: December 2015

AbstractSome title benzodiazepine derivatives are found to exhibit a broad spectrum of antibacterial activity and potency with respect to standard drugs streptomycin and ciprofloxacin.
ChemInform Abstract: Metal‐Free Intramolecular Alkyne‐Azide Cycloaddition to Construct the Pyrazolo[4,3‐f][1,2,3]triazolo[5,1‐c][1,4]oxazepine Ring System.
Authors: Arbaciauskiene Egle , Laukaityte Vaida , Holzer Wolfgang , Sackus Algirdas 
Published: December 2015

AbstractA simple and efficient synthetic route to a new pyrazolotriazolooxazepine ring system is developed by employing a metal‐free, intramolecular alkyne‐azide cycloaddition reaction as the key step.
ChemInform Abstract: Synthesis and Suzuki Reactions of N‐Heterocyclic Carbene Difluoro(aryl)‐boranes.
Authors: Nerkar Swapnil , Curran Dennis P. 
Published: December 2015

AbstractStable difluoro(aryl) boranes [e.g. (II)] are synthesized from NHC‐arylboranes [e.g. (I)] and Selectfluor in high yields and are a new class of stable precursors for Suzuki coupling.
ChemInform Abstract: Direct Synthesis of β‐Ketophosphonates and Vinyl Phosphonates from Alkenes or Alkynes Catalyzed by CuNPs/ZnO.
Authors: Gutierrez Victoria , Mascaro Evangelina , Alonso Francisco , Moglie Yanina , Radivoy Gabriel 
Published: December 2015

AbstractIt is found that alkynes conjugated with an aromatic ring or a carbon‐carbon double bond afford β‐ketophosponates as main products, whereas aliphatic alkynes or alkynes conjugated with a carbonyl group afford the corresponding vinyl phosphonates as mixtures of E/Z‐isomers.
ChemInform Abstract: Fe(III) Catalyzed Enantioselective Hydrophosphonylation of Aldehydes Promoted by Chiral Camphor Schiff Bases.
Authors: Xu Feng , Liu Yanpeng , Tu Jingxuan , Lei Chao , Li Gaoqiang 
Published: December 2015

AbstractNovel camphor‐derived Schiff bases prove to be efficient ligands for the iron(III)‐catalyzed hydrophosphonylation of aliphatic and aromatic aldehydes.
ChemInform Abstract: Three Minor New Compounds from the Aerial Parts of Leonurus japonicus.
Authors: Zhong Wei‐Mao , Cui Zhao‐Meng , Liu Zhi‐Ke , Yang Yan , Wu Da‐Rong , Liu Shao‐Hua , Long Hui , Sun Han‐Dong , Dang Yong‐Jun , Xiao Wei‐Lie 
Published: December 2015

AbstractA labdane‐type diterpenoid, leojaponin D (I), and two ionone derivatives, leojaponones A and B [(II) and (III)], are isolated from the aerial parts of Leonurus japonicus.
ChemInform Abstract: Spiroplakortone, an Unprecedented Spiroketal Lactone from the Chinese Sponge Plakortis simplex.
Authors: Chianese Giuseppina , Gu Bin‐Bin , Yang Fan , Jiao Wei‐Hua , Guo Yue‐Wei , Lin Hou‐Wen , Taglialatela‐Scafati Orazio 
Published: December 2015

AbstractA plausible pathway for the biosynthesis of the title compound (I) is also proposed.
Nucleic Acid Bioconjugates in Cancer Detection and Therapy
Authors: Patel Pradeepkumar L. , Rana Niki K. , Patel Mayurbhai R. , Kozuch Stephen D. , Sabatino David 
Published: December 2015

AbstractNucleoside‐ and nucleotide‐based chemotherapeutics have been used to treat cancer for more than 50 years. However, their inherent cytotoxicities and the emergent resistance of tumors against treatment has inspired a new wave of compounds in which the overall pharmacological profile of the bioactive nucleic acid component is improved by conjugation with delivery vectors, small‐molecule drugs, and/or imaging modalities. In this manner, nucleic acid bioconjugates have the potential for targeting and effecting multiple biological processes in tumors, leading to synergistic antitumor effects. Consequently, tumor resistance and recurrence is mitigated, leading to more effective forms of cancer therapy. Bioorthogonal chemistry has led to the development of new nucleoside bioconjugates, which have served to improve treatment efficacy en route towards FDA approval. Similarly, oligonucleotide bioconjugates have shown encouraging preclinical and clinical results. The modified oligonucleotides and their pharmaceutically active formulations have addressed many weaknesses of oligonucleotide‐based drugs. They have also paved the way for important advancements in cancer diagnosis and treatment. Cancer‐targeting ligands such as small‐molecules, peptides, and monoclonal antibody fragments have all been successfully applied in oligonucleotide bioconjugation and have shown promising anticancer effects in vitro and in vivo. Thus, the application of bioorthogonal chemistry will, in all likelihood, continue to supply a promising pipeline of nucleic acid bioconjugates for applications in cancer detection and therapy.