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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38条记录   Potent Farnesyltransferase Inhibitors with 1,4-Diazepane Scaffolds as Novel Destabilizing Microtubule Agents in Hormone-Resistant Prostate Cancer [作者：WLODARCZYK NICOLAS; LE BROCRYCKEWAERT DELPHINE; GILLERON PAULINE; LEMOINE AMELIE; FARCE AMAURY; CHAVATTE PHILIPPE; DUBOIS JOELLE; POMMERY NICOLE; HENICHART JEANPIERRE; FURMAN CHRISTOPHE; MILLET REGIS,期刊：Journal of Medicinal Chemistry, 页码：1178-1190 , 文章类型： Article，,卷期：2011年54-5] A new class of potent farnesyltransferase inhibitors based on a 1,4-diazepane scaffold was synthesized with protein farnesyltransferase inhibition potencies in the low nanomolar range. The compounds block the growth on t... Synthesis and Biological Evaluation of Orally Active Prodrugs of Indomethacin [作者：BANDGAR BABASAHEB P; SARANGDHAR RAJENDRA JANARDAN; VISWAKARMA SANTOSH; AHAMED FAKRUDEEN ALI,期刊：Journal of Medicinal Chemistry, 页码：1191-1201 , 文章类型： Article，,卷期：2011年54-5] Synthesis and biological evaluation of orally active prodrugs (1a-d) of indomethacin are described. Prodrugs 1a-c showed a similar degree of anti-inflammatory activity, and prodrug 1d was found to be less potent than the... Synthesis, Characterization, and Biological Evaluation of Novel Diclofenac Prodrugs [作者：BANDGAR BABASAHEB P; SARANGDHAR RAJENDRA JANARDAN; AHAMED FAKRUDEEN ALI; VISWAKARMA SANTOSH,期刊：Journal of Medicinal Chemistry, 页码：1202-1210 , 文章类型： Article，,卷期：2011年54-5] Diclofenac ester prodrugs (4, 5, 6) were synthesized and evaluated in vitro and in vivo for their potential use for oral delivery, with the aim of obtaining enzymatically labile and less ulceration drugs than the parent ... Discovery of Potent Inhibitors of Soluble Epoxide Hydrolase by Combinatorial Library Design and Structure-Based Virtual Screening [作者：XING LI; MCDONALD JOSEPH J; KOLODZIEJ STEVE A; KURUMBAIL RAVI G; WILLIAMS JENNIFER M; WARREN CHAD J; ONEAL JANET M; SKEPNER JILL E; ROBERDS STEVEN L,期刊：Journal of Medicinal Chemistry, 页码：1211-1222 , 文章类型： Article，,卷期：2011年54-5] Structure-based virtual screening was applied to design combinatorial libraries to discover novel and potent soluble epoxide hydrolase (sEH) inhibitors. X-ray crystal structures revealed unique interactions for a benzoxa... Evolution of Potent and Stable Placental-Growth-Factor-1-Targeting CovX-Bodies from Phage Display Peptide Discovery [作者：BOWER KRISTEN E; LAM SON N; OATES BRYAN D; DEL ROSARIO JOSELYN R; CORNER EMILY; OSOTHPRAROP TRINA F; KINHIKAR ARVIND G; HOYE JULIE A; PRESTON R RYAN; MURPHY ROBERT E; CAMPBELL LIOUDMILA A; HUANG HANHUA; JIMENEZ JUDITH; CAO XIA; CHEN GANG; AINEKULU ZEMEDA W; DATT AAKASH B; LEVIN NANCY J; DOPPALAPUDI VENKATA R; PIRIESHEPHERD STEVEN R; BRADSHAW CURT; WOODNUTT GARY; LAPPE RODNEY W,期刊：Journal of Medicinal Chemistry, 页码：1256-1265 , 文章类型： Article，,卷期：2011年54-5] Novel phage-derived peptides are the first reported molecules specifically targeting human placental growth factor 1 (P1GF-1). Phage data enabled peptide modifications that decreased IC50 values in PlGF-1/VEGFR-1 competi... Sugar-Based Enantiomeric and Conformationally Constrained Pyrrolo[2,1-c][1,4]-Benzodiazepines as Potential GABA(A) Ligands [作者：ARAUJO ANA C; RAUTER AMELIA P; NICOTRA FRANCESCO; AIROLDI CRISTINA; COSTA BARBARA; CIPOLLA LAURA,期刊：Journal of Medicinal Chemistry, 页码：1266-1275 , 文章类型： Article，,卷期：2011年54-5] Synthesis of a library of pyrrolo[2,1-c][1,4]-benzodiazepines derived from spiro bicyclic D- or L-proline analogues containing a D- or L-fructose moiety was developed. The L-fructose moiety was obtained by using a new sy... Design, Synthesis, and Structure-Activity Relationship of Trypanosoma brucei Leucyl-tRNA Synthetase Inhibitors as Antitrypanosomal Agents [作者：DING DAZHONG; MENG QINGQING; GAO GUANGWEI; ZHAO YAXUE; WANG QING; NARE BAKELA; JACOBS ROBERT; ROCK FERNANDO; ALLEY MICHAEL R K; PLATTNER JACOB J; CHEN GUOQIANG; LI DAWEI; ZHOU HUCHEN,期刊：Journal of Medicinal Chemistry, 页码：1276-1287 , 文章类型： Article，,卷期：2011年54-5] African trypanosomiasis, caused by the protozoal pathogen Tlypanosoma brucei (T. brucei), is one of the most neglected tropical diseases that are in great need of new drugs. We report the design and synthesis of T. bruce... A Unified, Probabilistic Framework for Structure- and Ligand-Based Virtual Screening [作者：SWANN STEVEN L; BROWN SCOTT P; MUCHMORE STEVEN W; PATEL HETAL; MERTA PHILIP; LOCKLEAR JOHN; HAJDUK PHILIP J,期刊：Journal of Medicinal Chemistry, 页码：1223-1232 , 文章类型： Article，,卷期：2011年54-5] We present a probabilistic framework for interpreting structure-based virtual screening that returns a quantitative likelihood of observing bioactivity and can be quantitatively combined with ligand-based screening metho... Isoindolinone Inhibitors of the Murine Double Minute 2 (MDM2)-p53 Protein-Protein Interaction: Structure-Activity Studies Leading to Improved Potency [作者：HARDCASTLE IAN R; LIU JUNFENG; VALEUR ERIC; WATSON ANNA; AHMED SHAFIQ U; BLACKBURN TIMOTHY J; BENNACEUR KARIM; CLEGG WILLIAM; DRUMMOND CATHERINE; ENDICOTT JANE A; GOLDING BERNARD T; GRIFFIN ROGER J; GRUBER JAN; HAGGERTY KAREN; HARRINGTON ROSS W; HUTTON CLAIRE; KEMP STUART; LU XIACHONG; MCDONNELL JAMES M; NEWELL DAVID R; NOBLE MARTIN E M; PAYNE SARA L; REVILL CHARLOTTE H; RIEDINGER CHRISTIANE; XU QING; LUNEC JOHN,期刊：Journal of Medicinal Chemistry, 页码：1233-1243 , 文章类型： Article，,卷期：2011年54-5] Inhibition of the MDM2-p53 interaction has been shown to produce an antitumor effect, especially in MDM2 amplified tumors.. The isoindolinone scaffold has proved to be versatile for the discovery of MDM2-p53 antagonists.... Antitumor Agents. 284. New Desmosdumotin B Analogues with Bicyclic B-Ring as Cytotoxic and Antitubulin Agents [作者：NAKAGAWAGOTO KYOKO; WU PEICHI; LAI CHINYU; HAMEL ERNEST; ZHU HAO; ZHANG LIYING; KOZAKA TAKASHI; OHKOSHI EMIKA; GOTO MASUO; BASTOW KENNETH F; LEE KUOHSIUNG,期刊：Journal of Medicinal Chemistry, 页码：1244-1255 , 文章类型： Article，,卷期：2011年54-5] We previously reported that the biological activity of analogues of desmosdumotin B (1) was dramatically changed depending on the B-ring system. A naphthalene B-ring analogue 3 exerted potent in vitro activity against a ... Fluorinated N,N-Dialkylaminostilbenes for Wnt Pathway Inhibition and Colon Cancer Repression [作者：ZHANG WEN; SVIRIPA VITALIY; KRIL LILIIA M; CHEN XI; YU TIANXIN; SHI JIANDANG; RYCHAHOU PIOTR; EVERS B MARK; WATT DAVID S; LIU CHUNMING,期刊：Journal of Medicinal Chemistry, 页码：1288-1297 , 文章类型： Article，,卷期：2011年54-5] Colorectal cancer (CRC) is the second leading cause of cancer-related mortality in the United States. CRC is initiated by mutations of the tumor suppressor gene, adenomatous polyposis coli (APC), or beta-catenin gene. Th... Structure-Activity Relationship, Conformational and Biological Studies of Temporin L Analogues [作者：MANGONI MARIA LUISA; CAROTENUTO ALFONSO; AURIEMMA LUIGIA; SAVIELLO MARIA ROSARIA; CAMPIGLIA PIETRO; GOMEZMONTERREY ISABEL; MALFI STEFANIA; MARCELLINI LUDOVICA; BARRA DONATELLA; NOVELLINO ETTORE; GRIECO PAOLO,期刊：Journal of Medicinal Chemistry, 页码：1298-1307 , 文章类型： Article，,卷期：2011年54-5] Temporins are naturally occurring peptides with promising features, which could lead to the development of new drugs. Temporin-ITI (TL) is the strongest antimicrobial peptide, but it is toxic on human erythrocytes and th... Potent Agonists of the Protease Activated Receptor 2 (PAR(2)) [作者：BOITANO SCOTT; FLYNN ANDREA N; SCHULZ STEPHANIE M; HOFFMAN JUSTIN; PRICE THEODORE J; VAGNER JOSEF,期刊：Journal of Medicinal Chemistry, 页码：1308-1313 , 文章类型： Article，,卷期：2011年54-5] Novel peptidomimetic pharmacophores to PAR(2) were designed based on the known activating peptide SLIGRL-NH2. A set of 15 analogues was evaluated with a model cell line (16HBE14o-) that highly expresses PAR(2). Cells exp... Incorporation of a Bioactive Reverse-Turn Heterocycle into a Peptide Template Using Solid-Phase Synthesis To Probe Melanocortin Receptor Selectivity and Ligand Conformations by 2D H-1 NMR [作者：SINGH ANAMIKA; WILCZYNSKI ANDRZEJ; HOLDER JERRY R; WITEK RACHEL M; DIRAIN MARVIN L; XIANG ZHIMIN; EDISON ARTHUR S; HASKELLLUEVANO CARRIE,期刊：Journal of Medicinal Chemistry, 页码：1379-1390 , 文章类型： Article，,卷期：2011年54-5] By use of a solid-phase synthetic approach, a bioactive reverse turn heterocycle was incorporated into a cyclic peptide template to probe melanocortin receptor potency and ligand structural conformations. The five melano... Discovery of Novel and Potent Orally Active Calcium-Sensing Receptor Antagonists that Stimulate Pulselike Parathyroid Hormone Secretion: Synthesis and Structure-Activity Relationships of Tetrahydropyrazolopyrimidine Derivatives [作者：YOSHIDA MASATO; MORI AKIRA; KOTANI ETSUO; OKA MASAHIRO; MAKINO HARUHIKO; FUJITA HISASHI; BAN JUNKO; IKEDA YUKIHIRO; KAWAMOTO TOMOHIRO; GOTO MIKA; KIMURA HIROYUKI; BABA ATSUO; YASUMA TSUNEO,期刊：Journal of Medicinal Chemistry, 页码：1430-1440 , 文章类型： Article，,卷期：2011年54-5] As part of our research for novel calcium-sensing receptor (CaSR) antagonists that can function as oral bone anabolic agents, we recently reported the discovery of a tetrahydropyrazolopyrimidine derivative featuring adam... Synthesis of 2-(Substituted Phenyl)-3,5,5-trimethylmorpholine Analogues and Their Effects on Monoamine Uptake, Nicotinic Acetylcholine Receptor Function, and Behavioral Effects of Nicotine [作者：CARROLL F IVY; MURESAN ANA Z; BLOUGH BRUCE E; NAVARRO HERNAN A; MASCARELLA S WAYNE; EATON J BREK; HUANG XIAODONG; DAMAJ M IMAD; LUKAS RONALD J,期刊：Journal of Medicinal Chemistry, 页码：1441-1448 , 文章类型： Article，,卷期：2011年54-5] Toward development of smoking cessation aids superior to bupropion (2), we describe synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues 5a-5h and their effects on inhibition of dopamine, norepinephrin...