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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共21条记录   Vascular Endothelial Growth Factor (VEGF) Receptors: Drugs and New Inhibitors [作者：MUSUMECI FRANCESCA; RADI MARCO; BRULLO CHIARA; SCHENONE SILVIA,期刊：Journal of Medicinal Chemistry, 页码：10797-10822 , 文章类型： Article，,卷期：2012年55-24] The recent launch onto the market of five VEGFR inhibitors indicates the therapeutic value of these agents and the importance of the research in the field of angiogenesis inhibitors for future oncologic therapy. In this ... Small Molecules That Target Protein Misfolding [作者：GAVRIN LORI KRIM; DENNY RAJIAH ALDRIN; SAIAH EDDINE,期刊：Journal of Medicinal Chemistry, 页码：10823-10843 , 文章类型： Article，,卷期：2012年55-24] Protein misfolding is a process in which proteins are unable to attain or maintain their biologically active conformation. Factors contributing to protein misfolding include missense mutations and intracellular factors s... Identification, Synthesis, and Biological Evaluation of Metabolites of the Experimental Cancer Treatment Drugs Indotecan (LMP400) and Indimitecan (LMP776) and Investigation of Isomerically Hydroxylated Indenoisoquinoline Analogues as Topoisomerase I Poisons [作者：CINELLI MANS A; REDDY P V NARASIMHA; LV PENGCHENG; LIANG JIANHUA; CHEN LIAN; AGAMA KELI; POMMIER YVES; VAN BREEMEN RICHARD B; CUSHMAN MARK,期刊：Journal of Medicinal Chemistry, 页码：10844-10862 , 文章类型： Article，,卷期：2012年55-24] Hydroxylated analogues of the anticancer topoisomerase I (Top1) inhibitors indotecan (LMP400) and indimitecan (LMP776) have been prepared because (1) a variety of potent Top1 poisons are known that contain strategically ... Design, Synthesis, and Biological Evaluation of Novel Deguelin-Based Heat Shock Protein 90 (HSP90) Inhibitors Targeting Proliferation and Angiogenesis [作者：CHANG DONGJO; AN HONGCHAN; KIM KYOUNGSUK; KIM HYUN HO; JUNG JINKYUNG; LEE JUNG MIN; KIM NAMJUNG; HAN YOUNG TAEK; YUN HWAYOUNG; LEE SUJIN; LEE GEUMWOO; LEE SEUNGBEOM; LEE JU SUNG; CHA JONGHO; PARK JIHYEON; PARK JI WON; LEE SUCHAN; KIM SANG GEON; KIM JEONG HUN; LEE HOYOUNG; KIM KYUWON; SUH YOUNGGER,期刊：Journal of Medicinal Chemistry, 页码：10863-10884 , 文章类型： Article，,卷期：2012年55-24] Deguelin exhibits potent apoptotic and antiangiogenic activities in a variety of transformed cells and cancer cells. Deguelin also exhibits potent tumor suppressive effects in xenograft tumor models for many human cancer... De Novo Cyclic Pseudopeptides Containing Aza-beta(3)-amino Acids Exhibiting Antimicrobial Activities [作者：LAURENCIN MATHIEU; AMOR MOSBAH; FLEURY YANNICK; BAUDYFLOCH MICHELE,期刊：Journal of Medicinal Chemistry, 页码：10885-10895 , 文章类型： Article，,卷期：2012年55-24] De novo cyclic pseudopeptides composed of alpha-amino and aza-beta(3)-amino acids were designed with the aim to obtain potential new antimicrobial agents. Antimicrobial cyclic pseudopeptides (ACPPs) are based on the prop... Coumarin-Based Inhibitors of Bacillus anthracis and Staphylococcus aureus Replicative DNA Helicase: Chemical Optimization, Biological Evaluation, and Antibacterial Activities [作者：LI BING; PAI RAMDAS; DI MING; AIELLO DANIEL; BARNES MARJORIE H; BUTLER MICHELLE M; TASHJIAN TOMMY F; PEET NORTON P; BOWLIN TERRY L; MOIR DONALD T,期刊：Journal of Medicinal Chemistry, 页码：10896-10908 , 文章类型： Article，,卷期：2012年55-24] The increasing prevalence of drug-resistant bacterial infections demands the development of new antibacterials that are not subject to existing mechanisms of resistance. Previously, we described coumarin-based inhibitors... Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors [作者：DEPREZPOULAIN REBECCA; FLIPO MARION; PIVETEAU CATHERINE; LEROUX FLORENCE; DASSONNEVILLE SANDRINE; FLORENT ISABELLE; MAES LOUIS; COS PAUL; DEPREZ BENOIT,期刊：Journal of Medicinal Chemistry, 页码：10909-10917 , 文章类型： Article，,卷期：2012年55-24] Malaria is a severe infectious disease that causes between 655 000 and 1.2 million deaths annually. To overcome the resistance to current drugs, new biological targets are needed for drug development. Aminopeptidase M1 (... Structural Investigation of Anti-Trypanosoma cruzi 2-Iminothiazolidin-4-ones Allows the Identification of Agents with Efficacy in Infected Mice [作者：MAGALHAES MOREIRA DIOGO RODRIGO; MANSO COSTA SALVANA PRISCYLLA; HERNANDES MARCELO ZALDINI; RABELLO MARCELO MONTENEGRO; DE OLIVEIRA FILHO GEVANIO BEZERRA; LAGOS DE MELO CRISTIANE MOUTINHO; DA ROCHA LUCAS FERREIRA; DE SIMONE CARLOS ALBERTO; FERREIRA RAFAELA SALGADO; BARBOSA FRADICO JORDANA RODRIGUES; MEIRA CASSIO SANTANA; GUIMARAES ELISALVA TEIXEIRA; SRIVASTAVA RAJENDRA MOHAN; ALVES PEREIRA VALERIA REGO; PEREIRA SOARES MILENA BOTELHO; LIMA LEITE ANA CRISTINA,期刊：Journal of Medicinal Chemistry, 页码：10918-10936 , 文章类型： Article，,卷期：2012年55-24] We modified the thiazolidinic ring at positions N3, C4, and C5, yielding compounds 6-24. Compounds with a phenyl at position N3, 15-19, 22-24, exhibited better inhibitory properties for cruzain and against the parasite t... Discovery of Salermide-Related Sirtuin Inhibitors: Binding Mode Studies and Antiproliferative Effects in Cancer Cells Including Cancer Stem Cells [作者：ROTILI DANTE; TARANTINO DOMENICO; NEBBIOSO ANGELA; PAOLINI CHANTAL; HUIDOBRO COVADONGA; LARA ESTER; MELLINI PAOLO; LENOCI ALESSIA; PEZZI RICCARDO; BOTTA GIORGIA; LAHTELAKAKKONEN MAIJA; POSO ANTTI; STEINKUEHLER CHRISTIAN; GALLINARI PAOLA; DE MARIA RUGGERO; FRAGA MARIO; ESTELLER MANEL; ALTUCCI LUCIA; MAI ANTONELLO,期刊：Journal of Medicinal Chemistry, 页码：10937-10947 , 文章类型： Article，,卷期：2012年55-24] Chemical changes performed on 1a (sirtinol) led to a series of SIRT1/2 inhibitors, in some cases more potent than la mainly against SIRT1. Tested in human leukemia U937 cells, the benzamide and anilide derivatives 1b, 1c... Synthesis and Evaluation of alpha-Thymidine Analogues as Novel Antimalarials [作者：CUI HUAQING; CARREROLERIDA JUANA; SILVA ANA P G; WHITTINGHAM JEAN L; BRANNIGAN JAMES A; RUIZPEREZ LUIS M; READ KEVIN D; WILSON KEITH S; GONZALEZPACANOWSKA DOLORES; GILBERT IAN H,期刊：Journal of Medicinal Chemistry, 页码：10948-10957 , 文章类型： Article，,卷期：2012年55-24] Plasmodium falciparum thymidylate kinase (PfTMPK) is a key enzyme in pyrimidine nucleotide biosynthesis. 3-Trifluoromethyl-4-chloro-phenyl-urea-alpha-thymidine has been reported as an inhibitor of Mycobacterium tuberculo... Potent, Selective, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin Kinase Domain Exhibiting Single Agent Antiproliferative Activity [作者：KOEHLER MICHAEL F T; BERGERON PHILIPPE; BLACKWOOD ELIZABETH; BOWMAN KRISTA K; CHEN YUNGHSIANG; DESHMUKH GAURI; DING XIAO; EPLER JENNIFER; LAU KEVIN; LEE LESLIE; LIU LICHUAN; LY CUONG; MALEK SHIVA; NONOMIYA JIM; OEH JASON; ORTWINE DANIEL F; SAMPATH DEEPAK; SIDERIS STEVE; TRINH LAN; TRUONG TOM; WU JIANSHENG; PEI ZHONGHUA; LYSSIKATOS JOSEPH P,期刊：Journal of Medicinal Chemistry, 页码：10958-10971 , 文章类型： Article，,卷期：2012年55-24] Selective inhibitors of mammalian target of rapamycin (mTOR) kinase based upon saturated heterocycles fused to a pyrimidine core were designed and synthesized. Each series produced compounds with K-i < 10 nM for the mTOR... Discovery of 6,7-Dihydro-5H-pyrrolo[2,3-a]pyrimidines as Orally Available G Protein-Coupled Receptor 119 Agonists [作者：KATAMREDDY SUBBA R; CARPENTER ANDREW J; AMMALA CARINA E; BOROS ERIC E; BRASHEAR RON L; BRISCOE CELIA P; BULLARD SARAH R; CALDWELL RICHARD D; CONLEE CHRISTOPHER R; CROOM DALLAS K; HART SHANE M; HEYER DENNIS O; JOHNSON PAUL R; KASHATUS JENNIFER A; MINICK DOUG J; PECKHAM GREGORY E; ROSS SEAN A; ROLLER SHANE G; SAMANO VICENTE A; SAULS HOWARD R; TADEPALLI SARVA M; THOMPSON JAMES B; XU YUN; WAY JAMES M,期刊：Journal of Medicinal Chemistry, 页码：10972-10994 , 文章类型： Article，,卷期：2012年55-24] GPR119 is a 7-transmembrane receptor that is expressed in the enteroendocrine cells in the intestine and in the islets of Langerhans in the pancreas. Indolines and 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines were discovered... Peptido Sulfonyl Fluorides as New Powerful Proteasome Inhibitors [作者：BROUWER ARWIN J; JONKER ANIKA; WERKHOVEN PAUL; KUO ETHAN; LI NAN; GALLASTEGUI NEREA; KERNMINK JOHAN; FLOREA BOGDAN I; GROLL MICHAEL; OVERKLEEFT HERMAN S; LISKAMP ROB M J,期刊：Journal of Medicinal Chemistry, 页码：10995-11003 , 文章类型： Article，,卷期：2012年55-24] A new class of potent proteasome inhibitors is described, of which the members contain an amino acid inspired sulfonyl fluoride as the electrophilic trap. In total, 24 peptido sulfonyl fluoride inhibitors have been desig... Effect of the Prosthetic Group on the Pharmacologic Properties of F-18-Labeled Rhodamine B, a Potential Myocardial Perfusion Agent for Positron Emission Tomography (PET) [作者：BARTHOLOMAE MARK D; GOTTUMUKKALA VIJAY; ZHANG SHAOHUI; BAKER AMANDA; DUNNING PATRICIA; FAHEY FREDERIC H; TREVES S TED; PACKARD ALAN B,期刊：Journal of Medicinal Chemistry, 页码：11004-11012 , 文章类型： Article，,卷期：2012年55-24] We recently reported the development of the 2-[F-18]fluoroethyl ester of rhodamine B as a potential positron emission tomography (PET) tracer for myocardial perfusion imaging. This compound, which was prepared using a [F... Dual Targeting of Hypoxic and Acidic Tumor Environments with a Cobalt(III) Chaperone Complex [作者：YAMAMOTO NATSUHO; RENFREW ANNA K; KIM BYUNG J; BRYCE NICOLE S; HAMBLEY TREVOR W,期刊：Journal of Medicinal Chemistry, 页码：11013-11021 , 文章类型： Article，,卷期：2012年55-24] The rational design of prodrugs for selective accumulation and activation in tumor microenvironments is one of the most promising strategies for minimizing the toxicity of anticancer drugs. Manipulation of the charge of ... Structure-Activity Relationship Studies of Orally Active Antimalarial 3,5-Substituted 2-Aminopyridines [作者：CABRERA DIEGO GONZALEZ; DOUELLE FREDERIC; YOUNIS YASSIR; FENG TZUSHEAN; LE MANACH CLAIRE; NCHINDA ALOYSIUS T; STREET LESLIE J; SCHEURER CHRISTIAN; KAMBER JOLANDA; WHITE KAREN L; MONTAGNAT OLIVER D; RYAN EILEEN; KATNENI KASIRAM; ZABIULLA K MOHAMMED; JOSEPH JAYAN T; BASHYAM SRIDEVI; WATERSON DAVID; WITTY MICHAEL J; CHARMAN SUSAN A; WITTLIN SERGIO; CHIBALE KELLY,期刊：Journal of Medicinal Chemistry, 页码：11022-11030 , 文章类型： Article，,卷期：2012年55-24] In an effort to address potential cardiotoxicity liabilities identified with earlier frontrunner compounds, a number of new 3,5-diaryl-2-aminopyridine derivatives were synthesized. Several compounds exhibited potent anti...