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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56条记录   Ethyl 8-Fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-car boxylate as Novel, Highly Potent, and Safe Antianxiety Agent. [作者：Anzini, Maurizio;Braile, Carlo;Valenti, Salvatore;Cappelli, Andrea;Vomero, Salvatore;Marinelli, Luciana;Limongelli, Vittorio;Novellino, Ettore;Betti, Laura;Giannaccini, Gino;Lucacchini, Antonio;Ghelardini, Carla;Norcini, Monica;Makovec, Francesco;Giorgi,,期刊：Journal of Medicinal Chemistry, 页码：4730-4743 , 文章类型： 研究论文，,卷期：2008年51-15] Et 8-fluoro-6-(4-nitrophenyl)- and Et 8-fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carb oxylate (I and II) were synthesized as central benzodiazepine receptor (CBR) ligands and tested for their abili... Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases. [作者：Wang, Tao;Lamb, Michelle L.;Scott, David A.;Wang, Haixia;Block, Michael H.;Lyne, Paul D.;Lee, John W.;Davies, Audrey M.;Zhang, Hai-Jun;Zhu, Yanyi;Gu, Fei;Han, Yongxin;Wang, Bin;Mohr, Peter J.;Kaus, Robert J.;Josey, John A.;Hoffmann, Ethan;Thress, Ken;MacI,期刊：Journal of Medicinal Chemistry, 页码：4672-4684 , 文章类型： 研究论文，,卷期：2008年51-15] The design, synthesis and biol. evaluation of a series of 4-(pyrazolylamino)pyrimidines I (R1 = H, Me, SMe, cyclopropyl, Me2CHO, n-PrO, Me3C; R2 = H, Br, Cl, F, Me; R3 = H, HOCH2CH2NH, (S)-HOCH2CH(OH)CH2NH, etc.; R4 = Me... Identification and Validation of Human DNA Ligase Inhibitors Using Computer-Aided Drug Design. [作者：Zhong, Shijun;Chen, Xi;Zhu, Xiao;Dziegielewska, Barbara;Bachman, Kurtis E.;Ellenberger, Tom;Ballin, Jeff D.;Wilson, Gerald M.;Tomkinson, Alan E.;MacKerell, Alexander D.;,期刊：Journal of Medicinal Chemistry, 页码：4553-4562 , 文章类型： 研究论文，,卷期：2008年51-15] Linking together of DNA strands by DNA ligases is essential for DNA replication and repair. Since many therapies used to treat cancer act by causing DNA damage, there is growing interest in the development of DNA repair... Discovery of 2-Chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a Potent Inducer of Apoptosis with High In Vivo Activity. [作者：Sirisoma, Nilantha;Kasibhatla, Shailaja;Pervin, Azra;Zhang, Hong;Jiang, Songchun;Willardsen, J. Adam;Anderson, Mark B.;Baichwal, Vijay;Mather, Gary G.;Jessing, Kevin;Hussain, Raouf;Hoang, Khanh;Pleiman, Christopher M.;Tseng, Ben;Drewe, John;Cai, Sui Xiong,期刊：Journal of Medicinal Chemistry, 页码：4771-4779 , 文章类型： 研究论文，,卷期：2008年51-15] Using a live cell, high-throughput caspase-3 activator assay, we have identified a novel series of 4-anilinoquinazolines as inducers of apoptosis. In this report, we discuss the discovery of 2-chloro-N-(4-methoxyphenyl)... The Effect of 5-Alkyl Modification on the Biological Activity of Pyrrolo[2,3-d]pyrimidine Containing Classical and Nonclassical Antifolates as Inhibitors of Dihydrofolate Reductase and as Antitumor and/or Antiopportunistic Infection Agents. [作者：Gangjee, Aleem;Jain, Hiteshkumar D.;Queener, Sherry F.;Kisliuk, Roy L.;,期刊：Journal of Medicinal Chemistry, 页码：4589-4600 , 文章类型： 研究论文，,卷期：2008年51-15] Compounds (More Than One Hetero Atom)) Section Novel classical antifolates (I, R = Pr, CHMe2) and 17 nonclassical antifolates (e.g. II) were synthesized as antitumor and/or antiopportunistic infection agents. Intermedia... Synthesis, Biological Evaluation, and Enzyme Docking Simulations of 1,5-Diarylpyrrole-3-Alkoxyethyl Ethers as Selective Cyclooxygenase-2 Inhibitors Endowed with Anti-inflammatory and Antinociceptive Activity. [作者：Anzini, Maurizio;Rovini, Michele;Cappelli, Andrea;Vomero, Salvatore;Manetti, Fabrizio;Botta, Maurizio;Sautebin, Lidia;Rossi, Antonietta;Pergola, Carlo;Ghelardini, Carla;Norcini, Monica;Giordani, Antonio;Makovec, Francesco;Anzellotti, Paola;Patrignani, Pao,期刊：Journal of Medicinal Chemistry, 页码：4476-4481 , 文章类型： 研究论文，,卷期：2008年51-15] A series of substituted 1,5-diaryl-3-(2-alkoxyethyl)pyrroles I (R1 = Ph, 4-FC6H4, 4-F3CC6H4; R2 = Me, Et, n-Pr) has been synthesized with the aim to assess if the replacement of the acetic ester moiety in the previously ... 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a Series of Anti-HIV-1 Agents of the Dihydro-alkoxy-benzyl-oxopyrimidine Family with Peculiar Structure-Activity Relationship Profile. [作者：Nawrozkij, Maxim B.;Rotili, Dante;Tarantino, Domenico;Botta, Giorgia;Eremiychuk, Alexandre S.;Musmuca, Ira;Ragno, Rino;Samuele, Alberta;Zanoli, Samantha;Armand-Ugon, Mercedes;Clotet-Codina, Imma;Novakov, Ivan A.;Orlinson, Boris S.;Maga, Giovanni;Este, Jos,期刊：Journal of Medicinal Chemistry, 页码：4641-4652 , 文章类型： 研究论文，,卷期：2008年51-15] A series of dihydro-alkylthio-benzyl-oxopyrimidines (S-DABOs) bearing a 2-aryl-2-oxoethylsulfanyl chain at pyrimidine C2, an alkyl group at C5, and a 2,6-dichloro-, 2-chloro-6-fluoro-, and 2,6-difluoro-benzyl substitutio... The Structural Basis for Peptidomimetic Inhibition of Eukaryotic Ribonucleotide Reductase: A Conformationally Flexible Pharmacophore. [作者：Xu, Hai;Fairman, James W.;Wijerathna, Sanath R.;Kreischer, Nathan R.;LaMacchia, John;Helmbrecht, Elizabeth;Cooperman, Barry S.;Dealwis, Chris;,期刊：Journal of Medicinal Chemistry, 页码：4653-4659 , 文章类型： 研究论文，,卷期：2008年51-15] Eukaryotic ribonucleotide reductase (RR) catalyzes nucleoside diphosphate conversion to deoxynucleoside diphosphate. Crucial for rapidly dividing cells, RR is a target for cancer therapy. RR activity requires formation... Discovery of a Novel Series of Benzoic Acid Derivatives as Potent and Selective Human b3 Adrenergic Receptor Agonists with Good Oral Bioavailability. Phenylethanolaminotetraline (PEAT) Skeleton Containing Biphenyl or Biphenyl Ether Moiety. [作者：Imanishi, Masashi;Nakajima, Yutaka;Tomishima, Yasuyo;Hamashima, Hitoshi;Washizuka, Kenichi;Sakurai, Minoru;Matsui, Shigeo;Imamura, Emiko;Ueshima, Koji;Yamamoto, Takao;Yamamoto, Nobuhiro;Ishikawa, Hirofumi;Nakano, Keiko;Unami, Naoko;Hamada, Kaori;Matsumura,期刊：Journal of Medicinal Chemistry, 页码：4804-4822 , 文章类型： 研究论文，,卷期：2008年51-15] biphenyl ether or biphenyl template on the RHS and a phenylethanolaminotetraline (PEAT) skeleton, which was prepd. by highly stereoselective synthesis, to generate two structurally different lead compds. (I, II) with a g... Design, Synthesis, and Antihepatocellular Carcinoma Activity of Nitric Oxide Releasing Derivatives of Oleanolic Acid. [作者：Chen, Li;Zhang, Yihua;Kong, Xiangwen;Lan, Edward;Huang, Zhangjian;Peng, Sixun;Kaufman, Daniel L.;Tian, Jide;,期刊：Journal of Medicinal Chemistry, 页码：4834-4838 , 文章类型： 研究论文，,卷期：2008年51-15] Novel furoxan-based nitric oxide (NO) releasing derivs. of oleanolic acid (OA) were synthesized for potential therapy of liver cancers. Six compds. produced high levels of NO in human hepatocellular carcinoma (HCC) cell... Naturally Occurring Homoisoflavonoids Function as Potent Protein Tyrosine Kinase Inhibitors by c-Src-Based High-Throughput Screening. [作者：Lin, Li-Gen;Xie, Hua;Li, Hong-Lin;Tong, Lin-Jiang;Tang, Chun-Ping;Ke, Chang-Qiang;Liu, Qun-Fang;Lin, Li-Ping;Geng, Mei-Yu;Jiang, Hualiang;Zhao, Wei-Min;Ding, Jian;Ye, Yang;,期刊：Journal of Medicinal Chemistry, 页码：4419-4429 , 文章类型： 研究论文，,卷期：2008年51-15] Protein tyrosine kinase (PTK) inhibitors represent emerging therapeutics for cancer chemoprevention. In our study, hematoxylin (26) was identified as one of the most remarkable c-Src inhibitors in an orthogonal compd.-m... Design, Synthesis, and Biological Evaluation of Antiviral Agents Targeting Flavivirus Envelope Proteins. [作者：Li, Ze;Khaliq, Mansoora;Zhou, Zhigang;Post, Carol Beth;Kuhn, Richard J.;Cushman, Mark;,期刊：Journal of Medicinal Chemistry, 页码：4660-4671 , 文章类型： 研究论文，,卷期：2008年51-15] Flavivirus envelope proteins (E proteins) have been shown to play a pivotal role in virus assembly, morphogenesis, and infection of host cells. Inhibition of flavivirus infection of a host cell by means of a small mol. ... Chemical Proteomics-Based Drug Design: Target and Antitarget Fishing with a Catechol-Rhodanine Privileged Scaffold for NAD(P)(H) Binding Proteins. [作者：Ge, Xia;Wakim, Bassam;Sem, Daniel S.;,期刊：Journal of Medicinal Chemistry, 页码：4571-4580 , 文章类型： 研究论文，,卷期：2008年51-15] Drugs typically exert their desired and undesired biol. effects by virtue of binding interactions with protein target(s) and antitarget(s), resp. Strategies are therefore needed to efficiently manipulate and monitor cros... A Pentacyclic Aurora Kinase Inhibitor (AKI-001) with High in Vivo Potency and Oral Bioavailability. [作者：Rawson, Thomas E.;Ruth, Matthias;Blackwood, Elizabeth;Burdick, Dan;Corson, Laura;Dotson, Jenna;Drummond, Jason;Fields, Carter;Georges, Guy J.;Goller, Bernhard;Halladay, Jason;Hunsaker, Thomas;Kleinheinz, Tracy;Krell, Hans-Willi;Li, Jun;Liang, Jun;Limberg,,期刊：Journal of Medicinal Chemistry, 页码：4465-4475 , 文章类型： 研究论文，,卷期：2008年51-15] Aurora kinase inhibitors have attracted a great deal of interest as a new class of antimitotic agents. We report a novel class of Aurora inhibitors based on a pentacyclic scaffold. A prototype pentacyclic inhibitor 32 ... Design, synthesis and biological evaluation of glutathione peptidomimetics as components of anti-parkinson prodrugs. [作者：More, Swati S.;Vince, Robert;,期刊：Journal of Medicinal Chemistry, 页码：4581-4588 , 文章类型： 研究论文，,卷期：2008年51-15] Plethoras of CNS-active drugs fail to effect their pharmacol. response due to their in vivo inability to cross the blood-brain barrier (BBB). The classical prodrug approach to overcome this frailty involves lipophilic d... (9S)-9-(2-Hydroxy-4,4-dimethyl-6-oxo-1-cyclohexen-1-yl)-3,3-dimethyl-2 ,3,4,9-tetrahydro-1H-xanthen-1-one, a Selective and Orally Active Neuropeptide Y Y5 Receptor Antagonist. [作者：Sato, Nagaaki;Jitsuoka, Makoto;Shibata, Takunobu;Hirohashi, Tomoko;Nonoshita, Katsumasa;Moriya, Minoru;Haga, Yuji;Sakuraba, Aya;Ando, Makoto;Ohe, Tomoyuki;Iwaasa, Hisashi;Gomori, Akira;Ishihara, Akane;Kanatani, Akio;Fukami, Takehiro;,期刊：Journal of Medicinal Chemistry, 页码：4765-4770 , 文章类型： 研究论文，,卷期：2008年51-15] (9S)-9-(2-Hydroxy-4,4-dimethyl-6-oxo-1-cyclohexen-1-yl)-3,3-dimethyl-2 ,3,4,9-tetrahydro-1H-xanthen-1-one ((S)-1) was identified as a selective and orally active neuropeptide Y Y5 receptor antagonist. The structure-acti...