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From Concept to Clinic [作者：FERRARIS DANA V,期刊：Journal of Medicinal Chemistry, 页码：4561-4584 , 文章类型： Article，,卷期：2010年53-12] Heat Shock Protein 70 (Hsp70) as an Emerging Drug Target [作者：EVANS CHRISTOPHER G; CHANG LYRA; GESTWICKI JASON E,期刊：Journal of Medicinal Chemistry, 页码：4585-4602 , 文章类型： Article，,卷期：2010年53-12] Selective GlyT1 Inhibitors: Discovery of [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a Promising Novel Medicine To Treat Schizophrenia [作者：PINARD EMMANUEL; ALANINE ALEXANDER; ALBERATI DANIELA; BENDER MARKUS; BORRONI EDILIO; BOURDEAUX PATRICK; BROM VIRGINIE; BURNER SERGE; FISCHER HOLGER; HAINZL DOMINIK; HALM REMY; HAUSER NICOLE; JOLIDON SYNESE; LENGYEL JUDITH; MARTY HANSPETER; MEYER THIERRY; MOREAU JEANLUC; MORY ROLAND; NARQUIZIAN ROBERT; NETTEKOVEN MATHIAS; NORCROSS ROGER D; PUELLMANN BERND; SCHMID PHILIPP; SCHMITT SEBASTIEN; STALDER HENRI; WERMUTH ROGER; WETTSTEIN JOSEPH G; ZIMMERLI DANIEL,期刊：Journal of Medicinal Chemistry, 页码：4603-4614 , 文章类型： Article，,卷期：2010年53-12] The GlyT1 transporter has emerged as a key novel target for the treatment of schizophrenia. Herein, we report on the optimization of the 2-alkoxy-5-methylsulfonebenzoylpiperazine class of GlyT1 inhibitors to improve hERG... Design of Selective, ATP-Competitive Inhibitors of Akt [作者：FREEMANCOOK KEVIN D; AUTRY CHRISTOPHER; BORZILLO GARY; GORDON DEBORAH; BARBACCITOBIN ELSA; BERNARDO VINCENT; BRIERE DAVID; CLARK TRACEY; CORBETT MATTHEW; JAKUBCZAK JOHN; KAKAR SHEFALI; KNAUTH ELIZABETH; LIPPA BLAISE; LUZZIO MICHAEL J; MANSOUR MAHMOUD; MARTINELLI GARY; MARX MATTHEW; NELSON KENDRA; PANDIT JAYVARDHAN; RAJAMOHAN FRANCIS; ROBINSON SHAUGHNESSY; SUBRAMANYAM CHAKRAPANI; WEI LIUQING; WYTHES MARTIN; MORRIS JOEL,期刊：Journal of Medicinal Chemistry, 页码：4615-4622 , 文章类型： Article，,卷期：2010年53-12] This paper describes the design and synthesis of novel, ATP-competitive Akt inhibitors from an elaborated 3-aminopyrrolidine scaffold. Key findings include the discovery of an initial lead that was modestly selective and... Identification and Functional Characterization of a Stable, Centrally Active Derivative of the Neurotensin (8-13) Fragment as a Potential First-in-Class Analgesic [作者：HUGHES FRANCIS M JR; SHANER BROOKE E; MAY LISA A; ZOTIAN LYNDSAY; BROWER JUSTIN O; WOODS R JEREMY; CASH MICHAEL; MORROW DUSTIN; MASSA FABIENNE; MAZELLA JEAN; DIX THOMAS A,期刊：Journal of Medicinal Chemistry, 页码：4623-4632 , 文章类型： Article，,卷期：2010年53-12] The neurotensin hexapapetide fragment NT(8-13) is a potent analgesic when administered directly to the central nervous system but does not cross the blood brain barrier. A total of 43 novel derivatives of NT(8-13) were e... Evaluation of Re and Tc-99m Complexes of 2-(4 '-Aminophenyl)benzothiazole as Potential Breast Cancer Radiopharmaceuticals [作者：TZANOPOULOU STAMATIA; SAGNOU MARINA; PARAVATOUPETSOTAS MARIA; GOURNI ELENI; LOUDOS GEORGE; XANTHOPOULOS STAVROS; LAFKAS DANIEL; KIARIS HIPPOKRATIS; VARVARIGOU ALEXANDRA; PIRMETTIS IOANNIS C; PAPADOPOULOS MINAS; PELECANOU MARIA,期刊：Journal of Medicinal Chemistry, 页码：4633-4641 , 文章类型： Article，,卷期：2010年53-12] The synthesis of M(I)(CO)(3)(NNO) (M = Re, Tc-99m) complexes conjugated to the antitumor agent 2-(4'-aminophenyl)benzothiazole and to its 6-methyl derivative, as well as their in vitro and in vivo biological evaluation a... Design and Synthesis of Novel Xyloketal Derivatives and Their Vasorelaxing Activities in Rat Thoracic Aorta and Angiogenic Activities in Zebrafish Angiogenesis Screen [作者：XU ZHONGLIANG; LI YIYING; XIANG QI; PEI ZHONG; LIU XILIN; LU BINGTAI; CHEN LING; WANG GUANLEI; PANG JIYAN; LIN YONGCHENG,期刊：Journal of Medicinal Chemistry, 页码：4642-4653 , 文章类型： Article，,卷期：2010年53-12] A novel series of xyloketal derivatives (1-21) were designed and prepared. The majority of the compounds demonstrated vasorelaxation action on 60 mM KCl-induced contractions rat isolated aortic rings in a concentration-d... Synthesis and Biological Characterization of the Histone Deacetylase Inhibitor Largazole and C7-Modified Analogues [作者：SOUTO JOSE A; VAZ ESTHER; LEPORE ILARIA; POEPPLER ANNCHRISTIN; FRANCI GIANLUIGI; ALVAREZ ROSANA; ALTUCCI LUCIA; DE LERA ANGEL R,期刊：Journal of Medicinal Chemistry, 页码：4654-4667 , 文章类型： Article，,卷期：2010年53-12] Largazole 4a and analogues with modifications at the C7 position, as well as 2,4'-bithiazole 5a, have been synthesized using an acyclic cross-metathesis of the corresponding depsipeptide structures assembled by N-C6(O) o... Novel Quinolizidinyl Derivatives as Antiarrhythmic Agents: 2. Further Investigation [作者：TASSO BRUNO; BUDRIESI ROBERTA; VAZZANA IANA; IOAN PIERFRANCO; MICUCCI MATTEO; NOVELLI FEDERICA; TONELLI MICHELE; SPARATORE ANNA; CHIARINI ALBERTO; SPARATORE FABIO,期刊：Journal of Medicinal Chemistry, 页码：4668-4677 , 文章类型： Article，,卷期：2010年53-12] Fifteen quinolizidine derivatives have been tested for antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig (gp) heart tissues and to assess calcium antagonist activity. All compounds exhibited from... Ruthenium-Porphyrin Conjugates with Cytotoxic and Phototoxic Antitumor Activity [作者：GIANFERRARA TERESA; BERGAMO ALBERTA; BRATSOS IOANNIS; MILANI BARBARA; SPAGNUL CINZIA; SAVA GIANNI; ALESSIO ENZO,期刊：Journal of Medicinal Chemistry, 页码：4678-4690 , 文章类型： Article，,卷期：2010年53-12] We report here two novel "extended-arms" porphyrins, TetbpyPP and TedabpyPP, in which four peripheral bpy fragments are connected to the meso positions of the macrocycle through flexible linkers of different length and h... Design, Synthesis, and Biological Evaluation of a Novel Class of gamma-Secretase Modulators with PPAR gamma Activity [作者：HIEKE MARTINA; NESS JULIA; STERI RAMONA; DITTRICH MICHAELA; GREINER CHRISTINE; WERZ OLIVER; BAUMANN KARLHEINZ; SCHUBERTZSILAVECZ MANFRED; WEGGEN SASCHA; ZETTL HEIKO,期刊：Journal of Medicinal Chemistry, 页码：4691-4700 , 文章类型： Article，,卷期：2010年53-12] We present a novel class of dual modulators of gamma-secretase and peroxisome proliferator-activated receptor gamma (PPAR gamma) based on the structure of 2-(bis(phenethoxy)pyrimidine-2-ylthio)hexanoic acid 8 (IC50(A bet... Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant [作者：HUANG WEISHENG; METCALF CHESTER A; SUNDARAMOORTHI RAJI; WANG YIHAN; ZOU DONG; THOMAS R MATHEW; ZHU XIAOTIAN; CAI LISI; WEN DAVID; LIU SHUANGYING; ROMERO JAN; QI JIWEI; CHEN INGRID; BANDA GEETHA; LENTINI SCOTT P; DAS SASMITA; XU QIHONG; KEATS JEFF; WANG FRANK; WARDWELL SCOTT; NING YAOYU; SNODGRASS JOSEPH T; BROUDY MARC I; RUSSIAN KARIN; ZHOU TIANJUN; COMMODORE LOIS; NARASIMHAN NARAYANA I; MOHEMMAD QURISH K; IULIUCCI JOHN; RIVERA VICTOR M; DALGARNO DAVID C; SAWYER TOMI K; CLACKSON TIM; SHAKESPEARE WILLIAM C,期刊：Journal of Medicinal Chemistry, 页码：4701-4719 , 文章类型： Article，,卷期：2010年53-12] In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the T315I gatekeeper mutant has emerged as resistant to all currently approved agents. This report describes the structure-guided design ... Online Fluorescence Enhancement Assay for the Acetylcholine Binding Protein with Parallel Mass Spectrometric Identification [作者：KOOL JEROEN; DE KLOE GERDIEN E; BRUYNEEL BEN; DE VLIEGER JON S; RETRA KIM; WIJTMANS MAIKEL; VAN ELK RENE; SMIT AUGUST B; LEURS ROB; LINGEMAN HENK; DE ESCH IWAN J P; IRTH HUBERTUS,期刊：Journal of Medicinal Chemistry, 页码：4720-4730 , 文章类型： Article，,卷期：2010年53-12] The acetylcholine binding protein (AChBP) is considered an analogue for the ligand-binding domain of neuronal nicotinic acetylcholine receptors (nAChRs). Its stability and solubility in aqueous buffer allowed the develop... Synthesis and Characterization of in Vitro and in Vivo Profiles of Hydroxybupropion Analogues: Aids to Smoking Cessation [作者：LUKAS RONALD J; MURESAN ANA Z; DAMAJ M IMAD; BLOUGH BRUCE E; HUANG XIAODONG; NAVARRO HERNAN A; MASCARELLA S WAYNE; EATON J BREK; MARXERMILLER SYNDIA K; CARROLL F IVY,期刊：Journal of Medicinal Chemistry, 页码：4731-4748 , 文章类型： Article，,卷期：2010年53-12] To create potentially superior aids to smoking cessation and/or antidepressants and to elucidate bupropion's possible mechanisms of action(s), 23 analogues based on its active hydroxymetabolite (2S,35)-4a were synthesize... Molecular Switch Controlling the Binding of Anionic Bile Acid Conjugates to Human Apical Sodium-Dependent Bile Acid Transporter [作者：RAIS RANA; ACHARYA CHAYAN; TRIRIYA GASIRAT; MACKERELL ALEXANDER D JR; POLLI JAMES E,期刊：Journal of Medicinal Chemistry, 页码：4749-4760 , 文章类型： Article，,卷期：2010年53-12] The human apical sodium-dependent bile acid transporter (hASBT) may serve as a prodrug target for oral drug absorption. Synthetic, biological, NMR, and computational approaches identified the structure activity relations... Synthesis, Biological Evaluation, and Structure-Activity Relationships of Dithiolethiones as Inducers of Cytoprotective Phase 2 Enzymes [作者：MUNDAY REX; ZHANG YUESHENG; PAONESSA JOSEPH D; MUNDAY CHRISTINE M; WILKINS ALISTAIR L; BABU JACOB,期刊：Journal of Medicinal Chemistry, 页码：4761-4767 , 文章类型： Article，,卷期：2010年53-12] Dithiolethiones are a family of promising cancer chemopreventive agents, and induction of phase 2 enzymes is key to their chemopreventive activities. Two dithiolethiones have been evaluated in humans for cancer preventio...