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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31条记录   Alcohol-, Diol-, and Carbohydrate-Substituted Indenoisoquinolines as Topoisomerase I Inhibitors: Investigating the Relationships Involving Stereochemistry, Hydrogen Bonding, and Biological Activity [作者：PETERSON KATHERINE E; CINELLI MARIS A; MORRELL ANDREW E; MEHTA AKHIL; DEXHEIMER THOMAS S; AGAMA KELI; ANTONY SMITHA; POMMIER YVES; CUSHMAN MARK,期刊：Journal of Medicinal Chemistry, 页码：4937-4953 , 文章类型： Article，,卷期：2011年54-14] The DNA-relaxing enzyme topoisomerase I (Top 1) can be inhibited by heterocyclic compounds such as indolocarbazoles and indenoisoquinolines. Carbohydrate and hydroxyl-containing side chains are essential for the biologic... Initial Efforts toward the Optimization of Arylomycins for Antibiotic Activity [作者：ROBERTS TUCKER C; SCHALLENBERGER MARK A; LIU JIAN; SMITH PETER A; ROMESBERG FLOYD E,期刊：Journal of Medicinal Chemistry, 页码：4954-4963 , 文章类型： Article，,卷期：2011年54-14] While most clinically used antibiotics were derived from natural products, the isolation of new broad-spectrum natural products has become increasingly rare and narrow-spectrum agents are typically deemed unsuitable for ... Design, Synthesis, and X-ray Crystallographic Studies of alpha-Aryl Substituted Fosmidomycin Analogues as Inhibitors of Mycobacterium tuberculosis 1-Deoxy-D-xylulose 5-Phosphate Reductoisomerase [作者：ANDALOUSSI MOUNIR; HENRIKSSON LENA M; WIECKOWSKA ANNA; LINDH MARTIN; BJORKELID CHRISTOFER; LARSSON ANNA M; SURESH SURISETTI; IYER HARINI; SRINIVASA BACHALLY R; BERGFORS TERESE; UNGE TORSTEN; MOWBRAY SHERRY L; LARHED MATS; JONES T ALWYN; KARLEN ANDERS,期刊：Journal of Medicinal Chemistry, 页码：4964-4976 , 文章类型： Article，,卷期：2011年54-14] The natural antibiotic fosmidomycin acts via inhibition of 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR), an essential enzyme in the non-mevalonate pathway of isoprenoid biosynthesis. Fosmidomycin is active on My... Regioselective Suzuki Coupling of Dihaloheteroaromatic Compounds as a Rapid Strategy To Synthesize Potent Rigid Combretastatin Analogues [作者：THEERAMUNKONG SEWAN; CALDARELLI ANTONIO; MASSAROTTI ALBERTO; APRILE SILVIO; CAPRIOGLIO DIEGO; ZANINETTI ROBERTA; TERUGGI ALESSIA; PIRALI TRACEY; GROSA GIORGIO; TRON GIAN CESARE; GENAZZANI ARMANDO A,期刊：Journal of Medicinal Chemistry, 页码：4977-4986 , 文章类型： Article，,卷期：2011年54-14] Combretastatin A-4 (CA-4) is a potent tubulin depolymerizing agent able to inhibit tumor growth and with antivascular effects. Although it is in clinical trials, the search for novel analogues that may display better/dif... Collateral Sensitivity of Multidrug-Resistant Cells to the Orphan Drug Tiopronin [作者：GOLDSBOROUGH ANDREW S; HANDLEY MISTY D; DULCEY ANDRES E; PLUCHINO KRISTEN M; KANNAN PAVITRA; BRIMACOMBE KYLE R; HALL MATTHEW D; GRIFFITHS GARY; GOTTESMAN MICHAEL M,期刊：Journal of Medicinal Chemistry, 页码：4987-4997 , 文章类型： Article，,卷期：2011年54-14] A major challenge in the treatment of cancer is multidrug resistance (MDR) that develops during chemotherapy. Here we demonstrate that tiopronin (1), a thiol-substituted N-propanoylglycine derivative, was selectively tox... Discovery of 1-{4[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyrida zin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl ]-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor [作者：MIWA KAZUHIRO; HITAKA TAKENORI; IMADA TAKASHI; SASAKI SATOSHI; YOSHIMATSU MIE; KUSAKA MASAMI; TANAKA AKIRA; NAKATA DAISUKE; FURUYA SHUICHI; ENDO SATOSHI; HAMAMURA KAZUMASA; KITAZAKI TOMOYUKI,期刊：Journal of Medicinal Chemistry, 页码：4998-5012 , 文章类型： Article，,卷期：2011年54-14] We previously discovered an orally active human gonadotropin-releasing hormone (GnRH) receptor antagonist, thieno[2,3-d] Pyrimidine-2,4-dione derivative 1 (sufugolix). To reduce the cytochrome P450 (CYP) inhibitory activ... N-Fused Imidazoles As Novel Anticancer Agents That Inhibit Catalytic Activity of Topoisomerase II alpha and Induce Apoptosis in G1/S Phase [作者：BAVISKAR ASHISH T; MADAAN CHETNA; PREET RANJAN; MOHAPATRA PURUSOTTAM; JAIN VAIBHAV; AGARWAL AMIT; GUCHHAIT SANKAR K; KUNDU CHANAKYA N; BANERJEE UTTAM C; BHARATAM PRASAD V,期刊：Journal of Medicinal Chemistry, 页码：5013-5030 , 文章类型： Article，,卷期：2011年54-14] On the basis of structures of known topoisomerase H catalytic inhibitors and initial molecular docking studies, bicyclic N-fused aminoimidazoles were predicted as potential topoisomerase II inihibitors. They were synthes... Discovery and SAR of Methylated Tetrahydropyranyl Derivatives as Inhibitors of Isoprenylcysteine Carboxyl Methyltransferase (ICMT) [作者：JUDD WESTON R; SLATTUM PAUL M; HOANG KHANH C; BHOITE LEENA; VALPPU LIISA; ALBERTS GLEN; BROWN BRITA; ROTH BRUCE; OSTANIN KIRILL; HUANG LIWEN; WETTSTEIN DANIEL; RICHARDS BURT; WILLARDSEN J ADAM,期刊：Journal of Medicinal Chemistry, 页码：5031-5047 , 文章类型： Article，,卷期：2011年54-14] A series of tetrahydropyranyl (THP) derivatives has been developed as potent inhibitors of isoprenylcysteine carboxyl methyltransferase (ICMT) for use as anticancer agents. Structural modification of the submicromolar hi... Hydrophilic Pyrazine Dyes as Exogenous Fluorescent Tracer Agents for Real-Time Point-of-Care Measurement of Glomerular Filtration Rate [作者：RAJAGOPALAN RAGHAVAN; NEUMANN WILLIAM L; POREDDY AMRUTA R; FITCH RICHARD M; FRESKOS JOHN N; ASMELASH BETHEL; GASTON KIMBERLY R; GALEN KAREN P; SHIEH JENGJONG; DORSHOW RICHARD B,期刊：Journal of Medicinal Chemistry, 页码：5048-5058 , 文章类型： Article，,卷期：2011年54-14] Various hydrophilic pyrazine-bis(carboxamides) derived from 3,5-diamino-pyrazine-2,5-dicarboxylic acid bearing neutral and anionic groups were prepared and evaluated for use as fluorescent glomerular filtration rate (GFR... Cytotoxic 1,2-Dialkynylimidazole-Based Aza-Enediynes: Aza-Bergman Rearrangement Rates Do Not Predict Cytotoxicity [作者：LAROCHE CHRISTOPHE; LI JING; KERWIN SEAN M,期刊：Journal of Medicinal Chemistry, 页码：5059-5069 , 文章类型： Article，,卷期：2011年54-14] A new class of potential antitumor agents inspired by the enediyne antitumor antibiotics has been synthesized: the 1,2-dialkynylimidazoles. The aza-Bergman rearrangement of these 1,2-dialkynylimidazoles has been investig... Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators [作者：HONG SANGPHYO; LIU KEVIN G; MA GIL; SABIO MICHAEL; UBERTI MICHELLE A; BACOLOD MARIA D; PETERSON JOHN; ZOU ZACK Z; ROBICHAUD ALBERT J; DOLLER DARIO,期刊：Journal of Medicinal Chemistry, 页码：5070-5081 , 文章类型： Article，,卷期：2011年54-14] There is an increasing amount of evidence to support that activation of the metabotropic glutamate receptor 4 (mGlu4 receptor), either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impact... Development of a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor (MK-8245) to Establish a Therapeutic Window for the Treatment of Diabetes and Dyslipidemia [作者：OBALLA RENATA M; BELAIR LIETTE; BLACK W CAMERON; BLEASBY KELLY; CHAN CHI CHUNG; DESROCHES CAROLE; DU XIAOBING; GORDON ROBERT; GUAY JOCELYNE; GUIRAL SEBASTIEN; HAFEY MICHAEL J; HAMELIN EMELIE; HUANG ZHENG; KENNEDY BRIAN; LACHANCE NICOLAS; LANDRY FRANCE; LI CHUN SING; MANCINI JOSEPH; NORMANDIN DENIS; POCAI ALESSANDRO; POWELL DAVID A; RAMTOHUL YEEMAN K; SKOREY KATHRYN; SORENSEN DAN; STURKENBOOM WAYNE; STYHLER ANGELA; WADDLETON DEENA M; WANG HAO; WONG SIMON; XU LIJING; ZHANG LEI,期刊：Journal of Medicinal Chemistry, 页码：5082-5096 , 文章类型： Article，,卷期：2011年54-14] The potential use of SCD inhibitors for the chronic treatment of diabetes and dyslipidemia has been limited by preclinical adverse events associated with inhibition of SCD in skin and eye tissues. To establish a therapeu... Antitumor Agents 288: Design, Synthesis, SAR, and Biological Studies of Novel Heteroatom-Incorporated Antofine and Cryptopleurine Analogues as Potent and Selective Antitumor Agents [作者：YANG XIAOMING; SHI QIAN; YANG SHUENNCHEN; CHEN CHIYUAN; YU SUNGLIANG; BASTOW KENNETH F; MORRISNATSCHKE SUSAN L; WU PEICHI; LAI CHINYU; WU TIANSHUNG; PAN SHIOWLIN; TENG CHEMING; LIN JAUCHEN; YANG PANCHYR; LEE KUOHSIUNG,期刊：Journal of Medicinal Chemistry, 页码：5097-5107 , 文章类型： Article，,卷期：2011年54-14] Novel heteroatom-incorporated antofine and cryptopleurine analogues were designed, synthesized, and tested against a panel of five cancer cell lines. Two new S-13-oxo analogues (11 and 16) exhibited potent cell growth in... Recognition of Drug Degradation Products by Target Proteins: Isotetracycline Binding to Tet Repressor [作者：VOLKERS GESA; PETRUSCHKA LOTHAR; HINRICHS WINFRIED,期刊：Journal of Medicinal Chemistry, 页码：5108-5115 , 文章类型： Article，,卷期：2011年54-14] Tetracycline antibiotics and their degradation products appear in medically treated tissues, food, soil, and manure sludge in the environment. In the context of protein interactions with various tetracyclines we performe... Imidazolopiperazines: Hit to Lead Optimization of New Antimalarial Agents [作者：WU TAO; NAGLE ADVAIT; KUHEN KELLI; GAGARING KERSTIN; BORBOA RACHEL; FRANCEK CAROLINE; CHEN ZHONG; PLOUFFE DAVID; GOH ANNE; LAKSHMINARAYANA SURESH B; WU JEANETTE; ANG HUI QING; ZENG PEITING; KANG MIN LOW; TAN WILLIAM; TAN MARIA; YE NICOLE; LIN XUENA; CALDWELL CHRISTOPHER; EK JARED; SKOLNIK SUZANNE; LIU FENGHUA; WANG JIANLING; CHANG JONATHAN; LI CHUN; HOLLENBECK THOMAS; TUNTLAND TOVE; ISBELL JOHN; FISCHLI CHRISTOPH; BRUN RETO; ROTTMANN MATTHIAS; DARTOIS VERONIQUE; KELLER THOMAS; DIAGANA THIERRY; WINZELER ELIZABETH; GLYNNE RICHARD; TULLY DAVID C; CHATTERJEE ARNAB K,期刊：Journal of Medicinal Chemistry, 页码：5116-5130 , 文章类型： Article，,卷期：2011年54-14] Starting from a hit series from a GNF compound library collection and based on a cell-based proliferation assay of Plasmodium falciparum, a novel imidazolopiperazine scaffold was optimized. SAR for this series of compoun... Selectivity of Kinase Inhibitor Fragments [作者：BAMBOROUGH PAUL; BROWN MURRAY J; CHRISTOPHER JOHN A; CHUNG CHUNWA; MELLOR GEOFF W,期刊：Journal of Medicinal Chemistry, 页码：5131-5143 , 文章类型： Article，,卷期：2011年54-14] A kinase-focused screening set of fragments has been assembled and has proved successful for the discovery of ligand-efficient hits against many targets. Here we present some of our general conclusions from this exercise...