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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63条记录   Discovery of Checkpoint Kinase Inhibitor (S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamid e (AZD7762) by Structure-Based Design and Optimization of Thiophenecarboxamide Ureas [作者：OZA VIBHA; ASHWELL SUSAN; ALMEIDA LYNSIE; BRASSIL PATRICK; BREED JASON; DENG CHUN; GERO THOMAS; GRONDINE MICHAEL; HORN CANDICE; IOANNIDIS STEPHANOS; LIU DONGFANG; LYNE PAUL; NEWCOMBE NICHOLAS; PASS MARTIN; READ JON; READY SHANNON; ROWSELL SIAN; SU MEI; TOADER DORIN; VASBINDER MELISSA; YU DINGWEI; YU YAN; XUE YAFENG; ZABLUDOFF SONYA; JANETKA JAMES,期刊：Journal of Medicinal Chemistry, 页码：5130-5142 , 文章类型： Article，,卷期：2012年55-11] Checkpoint kinases CHK1 and CHK2 are activated in response to DNA damage that results in cell cycle arrest, allowing sufficient time for DNA repair. Agents that lead to abrogation of such checkpoints have potential to in... Synthesis and Biological Evaluation of Derivatives of 2-{2-Fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic Acid: Nonsteroidal Anti-Inflammatory Drugs with Low Gastric Ulcerogenic Activity [作者：YAMAKAWA NAOKI; SUEMASU SHINTARO; OKAMOTO YOSHINARI; TANAKA KENICHIRO; ISHIHARA TOMOAKI; ASANO TEITA; MIYATA KEISHI; OTSUKA MASAMI; MIZUSHIMA TOHRU,期刊：Journal of Medicinal Chemistry, 页码：5143-5150 , 文章类型： Article，,卷期：2012年55-11] We previously reported that 2-fluoroloxoprofen has lower gastric ulcerogenic activity than loxoprofen, a nonsteroidal anti-inflammatory drug (NSAID) without selectivity for COX-2. We synthesized derivatives of 2-fluorolo... Rational Evolution of a Novel Type of Potent and Selective Proviral Integration Site in Moloney Murine Leukemia Virus Kinase 1 (PIM1) Inhibitor from a Screening-Hit Compound [作者：NAKANO HIROFUMI; SAITO NAE; PARKER LORIEN; TADA YUKIO; ABE MASANAO; TSUGANEZAWA KEIKO; YOKOYAMA SHIGEYUKI; TANAKA AKIKO; KOJIMA HIROTATSU; OKABE TAKAYOSHI; NAGANO TETSUO,期刊：Journal of Medicinal Chemistry, 页码：5151-5164 , 文章类型： Article，,卷期：2012年55-11] Serine/threonine kinase PIM1 is an emerging therapeutic target for hematopoietic and prostate cancer therapy. To develop a novel PIM1 inhibitor, we focused on 1, a metabolically labile, nonselective kinase inhibitor disc... The Experimental Uncertainty of Heterogeneous Public K-i Data [作者：KRAMER CHRISTIAN; KALLIOKOSKI TUOMO; GEDECK PETER; VULPETTI ANNA,期刊：Journal of Medicinal Chemistry, 页码：5165-5173 , 文章类型： Article，,卷期：2012年55-11] The maximum achievable accuracy of in silico models depends on the quality of the experimental data. Consequently, experimental uncertainty defines a natural upper limit to the predictive performance possible. Models tha... (Z)-1-Aryl-3-arylamino-2-propen-1-ones, Highly Active Stimulators of Tubulin Polymerization: Synthesis, Structure-Activity Relationship (SAR), Tubulin Polymerization, and Cell Growth Inhibition Studies [作者：REDDY M V RAMANA; AKULA BALAIAH; COSENZA STEPHEN C; LEE CLEMENT M; MALLIREDDIGARI MURALIDHAR R; PALLELA VENKAT R; SUBBAIAH D R C VENKATA; UDOFA ANDREW; REDDY E PREMKUMAR,期刊：Journal of Medicinal Chemistry, 页码：5174-5187 , 文章类型： Article，,卷期：2012年55-11] Tubulin, the major structural component of microtubules, is a target for the development of anticancer agents. A series of (Z)-1-aryl-3-arylamino-2-propen-1-one (10) were synthesized and evaluated for antiproliferative a... Structure-Based Design of a Novel Series of Potent, Selective Inhibitors of the Class I Phosphatidylinositol 3-Kinases [作者：SMITH ADRIAN L; DANGELO NOEL D; BO YURAIN Y; BOOKER SHON K; CEE VICTOR J; HERBERICH BRAD; HONG FANGTSAO; JACKSON CLAIRE L M; LANMAN BRIAN A; LIU LONGBIN; NISHIMURA NOBUKO; PETTUS LIPING H; REED ANTHONY B; TADESSE SEIFU; TAMAYO NURIA A; WURZ RYAN P; YANG KEVIN; ANDREWS KRISTIN L; WHITTINGTON DOUGLAS A; MCCARTER JOHN D; MIGUEL TISHA SAN; ZALAMEDA LEEANNE; JIANG JIAN; SUBRAMANIAN RAJU; MULLADY ERIN L; CAENEPEEL SEAN; FREEMAN DANIEL J; WANG LING; ZHANG NANCY; WU TIAN; HUGHES PAUL E; NORMAN MARK H,期刊：Journal of Medicinal Chemistry, 页码：5188-5219 , 文章类型： Article，,卷期：2012年55-11] A highly selective series of inhibitors of the class I phosphatidylinositol 3-kinases (PI3Ks) has been designed and synthesized. Starting from the dual PI3K/mTOR inhibitor 5, a structure-based approach was used to improv... Identification of a Novel Family of BRAF(V600E) Inhibitors [作者：QJN JIE; XIE PENG; VENTOCILLA CHRISTIAN; ZHOU GUOQIANG; VULTUR ADINA; CHEN QUAN; LIU QIN; HERLYN MEENHARD; WINKLER JEFFREY; MARMORSTEIN RONEN,期刊：Journal of Medicinal Chemistry, 页码：5220-5230 , 文章类型： Article，,卷期：2012年55-11] The BRAF oncoprotein is mutated in about half of malignant melanomas and other cancers, and a kinase activating single valine to glutamate substitution at residue 600 (BRAF(V600E)) accounts for over 90% of BRAF-mediated ... Tacrine-Silibinin Codrug Shows Neuro- and Hepato protective Effects in Vitro and Pro-Cognitive and Hepatoprotective Effects in Vivo [作者：CHEN XINYU; ZENGER KATHARINA; LUPP AMELIE; KLING BEATA; HEILMANN JOERG; FLECK CHRISTIAN; KRAUS BIRGIT; DECKER MICHAEL,期刊：Journal of Medicinal Chemistry, 页码：5231-5242 , 文章类型： Article，,卷期：2012年55-11] A codrug of the anti-Alzheimer drug tacrine and the natural product silibinin was synthesized. The codrug's biological and pharmacological properties were compared to an equimolar mixture of the components. The compound ... A Selective, Orally Bioavailable 1,2,4-Triazolo[1;5-a]pyridine-Based Inhibitor of Janus Kinase 2 for Use in Anticancer Therapy: Discovery of CEP-33779 [作者：DUGAN BENJAMIN J; GINGRICH DIANE E; MESAROS EUGEN F; MILKIEWICZ KAREN L; CURRY MATTHEW A; ZULLI ALLISON L; DOBRZANSKI PAWEL; SERDIKOFF CYNTHIA; JAN MAHFUZA; ANGELES THELMA S; ALBOM MARK S; MASON JENNIFER L; AIMONE LISA D; MEYER SHERYL L; HUANG ZEQI; WELLSKNECHT KEVIN J; ATOR MARK A; RUGGERI BRUCE A; DORSEY BRUCE D,期刊：Journal of Medicinal Chemistry, 页码：5243-5254 , 文章类型： Article，,卷期：2012年55-11] Members of the JAK family of nonreceptor tyrosine kinases play a critical role in the growth and progression of many cancers and in inflammatory diseases. JAK2 has emerged as a leading therapeutic target for oncology, pr... Synthesis and Structure-Activity Relationships of Pyrazolo[1,5-a]pyridine Derivatives: Potent and Orally Active Antagonists of Corticotropin-Releasing Factor 1 Receptor [作者：TAKAHASHI YOSHINORI; HIBI SHIGEKI; HOSHINO YORIHISA; KIKUCHI KOICHI; SHIN KOGYOKU; MURATATAI KAORU; FUJISAWA MASAE; INO MITSUHIRO; SHIBATA HISASHI; YONAGA MASAHIRO,期刊：Journal of Medicinal Chemistry, 页码：5255-5269 , 文章类型： Article，,卷期：2012年55-11] Design, synthesis, and structure activity relationships of a series of 3-dialkylamino-7-phenyl pyrazolo[1,5-a]pyridines (I) as selective antagonists of the corticotropin-releasing factor 1 (CRF1) receptor are described. ... Rational Design of 4-Aryl-1,2,3-Triazoles for Indoleamine 2,3-Dioxygenase 1 Inhibition [作者：ROEHRIG UTE F; MAJJIGAPU SOMI REDDY; GROSDIDIER AURELIEN; BRON SYLVIAN; STROOBANT VINCENT; PILOTTE LUC; COLAU DIDIER; VOGEL PIERRE; VAN DEN EYNDE BENOIT J; ZOETE VINCENT; MICHIELIN OLIVIER,期刊：Journal of Medicinal Chemistry, 页码：5270-5290 , 文章类型： Article，,卷期：2012年55-11] Indoleamine 2,3-dioxygenase 1 (IDO1) is an important therapeutic target treatment of diseases such as cancer that involve pathological immune escape. Starting from the scaffold of our previously discovered IDO1 inhibitor... Discovery and Optimization of a Series of 3-(3-Phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: Orally Bioavailable, Selective, and Potent ATP-Independent Akt Inhibitors [作者：ASHWELL MARK A; LAPIERRE JEANMARC; BRASSARD CHRISTOPHER; BRESCIANO KAREN; BULL CATHY; CORNELLKENNON SUSAN; EATHIRAJ SUDHARSHAN; FRANCE DENNIS S; HALL TERENCE; HILL JASON; KELLEHER EOIN; KHANAPURKAR SAMPADA; KIZER DARIN; KOERNER STEFFI; LINK JEFF; LIU YANBIN; MAKHIJA SAPNA; MOUSSA MAGDI; NAMDEV NIVEDITA; KHANH NGUYEN; NICEWONGER ROBERT; PALMA ROCIO; SZWAYA JEFF; TANDON MANISH; UPPALAPATI UMA; VENSEL DAVID; VOLAK LAURIE P; VOLCKOVA ERIKA; WESTLUND NEIL; WU HUI; YANG RUIYANG; CHAN THOMAS C K,期刊：Journal of Medicinal Chemistry, 页码：5291-5310 , 文章类型： Article，,卷期：2012年55-11] This paper describes the implementation of a biochemical and biophysical screening strategy to identify and optimize small molecule Akt1 inhibitors that act through a mechanism distinct from that observed for kinase doma... A Prospective Cross-Screening Study on G-Protein-Coupled Receptors: Lessons Learned in Virtual Compound Library Design [作者：SANDERS MARIJN P A; ROUMEN LUC; VAN DER HORST EELKE; LANE J ROBERT; VISCHER HENRY F; VAN OFFENBEEK JODY; DE VRIES HENK; VERHOEVEN STEFAN; CHOW KEN Y; VERKAAR FOLKERT; BEUKERS MARGOT W; MCGUIRE ROSS; LEURS ROB; IJZERMAN ADRIAAN P; DE VLIEG JACOB; DE ESCH IWAN J P; ZAMAN GUIDO J R; KLOMP JAN P G; BENDER ANDREAS; DE GRAAF CHRIS,期刊：Journal of Medicinal Chemistry, 页码：5311-5325 , 文章类型： Article，,卷期：2012年55-11] We present the systematic prospective evaluation of a protein-based and a ligand-based virtual screening platform against a set of three G-protein-coupled receptors (GPCRs): the beta-2 alrenoreceptor (ADRB2), the adenosi... In Vitro Anticancer Activity of cis-Diammineplatinum(II) Complexes with beta-Diketonate Leaving Group Ligands [作者：WILSON JUSTIN J; LIPPARD STEPHEN J,期刊：Journal of Medicinal Chemistry, 页码：5326-5336 , 文章类型： Article，,卷期：2012年55-11] Five cationic platinum(II) complexes of general formula, [Pt(NH3)(2-)(beta-diketonate)]X are reported, where X is a noncoordinating anion and beta-diketonate = acetylacetonate (acac), 1,1,1,-trifluoroacetylacetonate (tfa... Design, Synthesis, and Evaluation of 3,5-Disubstituted 7-Azaindoles as Trk Inhibitors with Anticancer and Antiangiogenic Activities [作者：HONG SEUNGHEE; KIM JINHEE; SEO JU HYEON; JUNG KYUNG HEE; HONG SOONSUN; HONG SUNGWOO,期刊：Journal of Medicinal Chemistry, 页码：5337-5349 , 文章类型： Article，,卷期：2012年55-11] Tropomyosin-related kinase A (TrkA) is considered a promising target in the development of a therapeutic treatment of cancer and pain. In this study, we designed and synthesized a series of novel 7-azaindole-based Trk ki...