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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   Design, Synthesis, and DNA-Binding of N-Alkyl(anilino)quinazoline Derivatives [作者：GAROFALO ANTONIO; GOOSSENS LAURENCE; BALDEYROU BRIGITTE; LEMOINE AMELIE; RAVEZ SEVERINE; SIX PERRINE; DAVIDCORDONNIER MARIEHELENE; BONTE JEANPAUL; DEPREUX PATRICK; LANSIAUX AMELIE; GOOSSENS JEANFRANCOIS,期刊：Journal of Medicinal Chemistry, 页码：8089-8103 , 文章类型： Article，,卷期：2010年53-22] New N-alkylanilinoquinazoline derivatives 5, 12, 20, and 22 have been prepared Crow 4-chloro-6, 7-dimethoxyquinazoline 3, 4-chloro-6,7-methylenedioxyquinazoline 19, and commercially available anilines. Differents classes... In Vivo Characterization of a Dual Adenosine A(2A)/A(1) Receptor Antagonist in Animal Models of Parkinson's Disease [作者：SHOOK BRIAN C; RASSNICK STEFANIE; OSBORNE MELVILLE C; DAVIS SCOTT; WESTOVER LORI; BOULET JAMIE; HALL DANIEL; RUPERT KENNETH C; HEINTZELMAN GEOFFREY R; HANSEN KRISTIN; CHAKRAVARTY DEVRAJ; BULLINGTON JAMES L; RUSSELL RONALD; BRANUM SHAWN; WELLS KENNETH M; DAMON SANDRA; YOUELLS SCOTT; LI XUN; BEAUCHAMP DEREK A; PALMER DAVID; REYES MAYRA; DEMAREST KEITH; TANG YUTING; RHODES KENNETH; JACKSON PAUL F,期刊：Journal of Medicinal Chemistry, 页码：8104-8115 , 文章类型： Article，,卷期：2010年53-22] The in vivo characterization of a dual adenosine A(2A)/A(1) I receptor antagonist in several animal models of Parkinson's disease is described. Discovery and scale-up syntheses of compound 1 are described in detail, high... Synthesis and Discovery of Water-Soluble Microtubule Targeting Agents that Bind to the Colchicine Site on Tubulin and Circumvent Pgp Mediated Resistance [作者：GANGJEE ALEEM; ZHAO YING; LIN LU; RAGHAVAN SUDHIR; ROBERTS ELIZABETH G; RISINGER APRIL L; HAMEL ERNEST; MOOBERRY SUSAN L,期刊：Journal of Medicinal Chemistry, 页码：8116-8128 , 文章类型： Article，,卷期：2010年53-22] Two classes of molecules were designed and synthesized based on a 6-CH3 cyclopenta[d]pyrimidine scaffold and a pyrrolo[2,3-d]pyrimidine scaffold. The pyrrolo[2,3-d]pyrimidines were synthesized by reacting ethyl 2-cyano-4... Assessment of Chemoselective Neoglycosylation Methods Using Chlorambucil as a Model [作者：GOFF RANDAL D; THORSON JON S,期刊：Journal of Medicinal Chemistry, 页码：8129-8139 , 文章类型： Article，,卷期：2010年53-22] To systematically assess the impact of glycosylation and the corresponding chemoselective linker upon the anticancer activity/selectivity of the drug chlorambucil, herein we report the synthesis and anticancer activities... Novel Potent Orally Active Multitargeted Receptor Tyrosine Kinase Inhibitors: Synthesis, Structure-Activity Relationships, and Antitumor Activities of 2-Indolinone Derivatives [作者：CHO TANG PENG; DONG SU YI; JUN FENG; HONG FU JIAN; LIANG YANG JIANG; LU XIAO; HUA PENG JIANG; LI LI YA; LEI ZHANG; BING HU; YING ZHOU; QIONG LI FANG; BEI FU BEI; GUANG LOU LI; SHEN GONG AI; HONG SHE GAO; HONG SUN WEI; TAI MONG XIAN,期刊：Journal of Medicinal Chemistry, 页码：8140-8149 , 文章类型： Article，,卷期：2010年53-22] The inhibition of receptor tyrosine kinases (RTKs) has become a successful approach in the development of anticancer agents. Many potent small-molecule kinase inhibitors have been discovered. We report herein a series of... 2 '-Deoxy-2 '-spirocyclopropylcytidine Revisited: A New and Selective Inhibitor of the Hepatitis C Virus NS5B Polymerase [作者：JONCKERS TIM H M; LIN TSEI; BUYCK CHRISTOPHE; LACHAUDURAND SOPHIE; VANDYEK KOEN; VAN HOOF STEVEN; VANDEKERCKHOVE LEEN A M; HU LILI; BERKE JAN MARTIN; VIJGEN LEEN; DILLEN LIEVE L A; CUMMINGS MAXWELL D; DE KOCK HERMAN; NILSSON MAGNUS; SUND CHRISTIAN; RYDEGARD CHRISTINA; SAMUELSSON BERTIL; ROSENQUIST ASA; FANNING GREGORY; VAN EMELEN KRISTOF; SIMMEN KENNETH; RABOISSON PIERRE,期刊：Journal of Medicinal Chemistry, 页码：8150-8160 , 文章类型： Article，,卷期：2010年53-22] The current therapy for hepatitis C virus (HCV) infection has limited efficacy, in particular against the genotype 1 virus, and a range of side effects. In this context of high unmet medical need, more efficacious drugs ... Design, Synthesis, and Biological Evaluation of Novel Hybrid Dicaffeoyltartaric/Diketo Acid and Tetrazole-Substituted L-Chicoric Acid Analogue Inhibitors of Human Immunodeficiency Virus Type 1 Integrase [作者：CROSBY DAVID C; LEI XIANGYANG; GIBBS CHARLES G; MCDOUGALL BRENDA R; ROBINSON W EDWARD JR; REINECKE MANFRED G,期刊：Journal of Medicinal Chemistry, 页码：8161-8175 , 文章类型： Article，,卷期：2010年53-22] Fourteen analogues of the anti-HIV-1 integrase (IN) inhibitor L-chicoric acid (L-CA) were prepared. Their IC50 values for 3'-end processing and strand transfer against recombinant HIV-1 IN were determined in vitro, and t... Bicyclic Substituted Hydroxyphenylmethanones as Novel Inhibitors of 17 beta-Hydroxysteroid Dehydrogenase Type 1 (17/beta-HSD1) for the Treatment of Estrogen-Dependent Diseases [作者：OSTER ALEXANDER; HINSBERGER STEFAN; WERTH RUTH; MARCHAISOBERWINKLER SANDRINE; FROTSCHER MARTIN; HARTMANN ROLF W,期刊：Journal of Medicinal Chemistry, 页码：8176-8186 , 文章类型： Article，,卷期：2010年53-22] Estradiol (E2), the most important estrogen in humans, is involved in the initiation and progression of estrogen-dependent diseases such as breast cancer and endometriosis. Its local production in the target cell is regu... Novel alpha 3 beta 4 Nicotinic Acetylcholine Receptor-Selective Ligands. Discovery, Structure-Activity Studies, and Pharmacological Evaluation [作者：ZAVERI NURULAIN; JIANG FAMING; OLSEN CRIS; POLGAR WILLMA; TOLL LAWRENCE,期刊：Journal of Medicinal Chemistry, 页码：8187-8191 , 文章类型： Article，,卷期：2010年53-22] Antagonist activity at the alpha 3 beta 4 nicotinic acetylcholine receptor (nAChR) is thought to contribute to the antiaddictive properties of several compounds. However, truly selective ligands for the alpha 3 beta 4 nA... Organometallic Osmium Arene Complexes with Potent Cancer Cell Cytotoxicity [作者：FU YING; HABTEMARIAM ABRAHA; PIZARRO ANA M; VAN RIJT SABINE H; HEALEY DAVID J; COOPER PATRICIA A; SHNYDER STEVEN D; CLARKSON GUY J; SADLER PETER J,期刊：Journal of Medicinal Chemistry, 页码：8192-8196 , 文章类型： Article，,卷期：2010年53-22] Iodido osmium(II) complexes [Os(eta(6)-arene)(XY)I](+) (XY = p-hydroxy or p-dimethylaminophenylazopyridine, arene = p-cymene or biphenyl) are potently cytotoxic at nanomolar concentrations toward a panel of human cancer ... Parallel Synthesis, Evaluation, and Preliminary Structure-Activity Relationship of 2,5-Diamino-1,4-benzoquinones as a Novel Class of Bivalent Anti-Prion Compound [作者：BONGARZONE SALVATORE; HOANG NGOC AI TRAN; CAVALLI ANDREA; ROBERTI MARINELLA; CARLONI PAOLO; LEGNAME GIUSEPPE; BOLOGNESI MARIA LAURA,期刊：Journal of Medicinal Chemistry, 页码：8197-8201 , 文章类型： Article，,卷期：2010年53-22] A library of 11 entries, featuring a 2,5-diamino-1,4-benzoquinones nucleus as spacer connecting two aromatic prion recognition motifs, was designed and evaluated against prion infection. Notably. 6-chloro-1,2,3,4-tetrith... Endoperoxide Carbonyl Falcipain 2/3 Inhibitor Hybrids: Toward Combination Chemotherapy of Malaria through a Single Chemical Entity [作者：GIBBONS PETER; VERISSIMO EDITE; ARAUJO NUNA C; BARTON VICTORIA; NIXON GEMMA L; AMEWU RICHARD K; CHADWICK JAMES; STOCKS PAUL A; BIAGINI GIANCARLO A; SRIVASTAVA ABHISHEK; ROSENTHAL PHILIP J; GUT JIRI; GUEDES RITA C; MOREIRA RUI; SHARMA RAMAN; BERRY NEIL; CRISTIANO M LUDES S; SHONE ALISON E; WARD STEPHEN A; ONEILL PAUL M,期刊：Journal of Medicinal Chemistry, 页码：8202-8206 , 文章类型： Article，,卷期：2010年53-22] We extend our approach of combination chemotherapy through a single prodrug entity (O'Neill et al. Angew. Chem., Int. Ed. 2004, 43, 4193) by using a 1,2,4-trioxolane as a protease inhibitor carbonyl-masking group. These ... Selective Hexapeptide Agonists and Antagonists for Human Complement C3a Receptor (vol 53, pg 4938, 2010) [作者：SCULLY CONOR C G; BLAKENEY JADE S; SINGH RANCE; HOANG HUY N; ABBENANTE GIOVANNI; REID ROBERT C; FAIRLIE DAVID P,期刊：Journal of Medicinal Chemistry, 页码：8208-8208 , 文章类型： Correction，,卷期：2010年53-22] Medicinal Chemistry of siRNA Delivery [作者：STANTON MATTHEW G; COLLETTI STEVEN L,期刊：Journal of Medicinal Chemistry, 页码：7887-7901 , 文章类型： Article，,卷期：2010年53-22] Nitrile-Containing Pharmaceuticals: Efficacious Roles of the Nitrile Pharmacophore [作者：FLEMING FRASER F; YAO LIHUA; RAVIKUMAR P C; FUNK LEE; SHOOK BRIAN C,期刊：Journal of Medicinal Chemistry, 页码：7902-7917 , 文章类型： Article，,卷期：2010年53-22]