个性化文献订阅>文章检索

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44条记录   Design, Synthesis, and Biological Evaluation of Potent c-Met Inhibitors. [作者：D'Angelo, Noel D.;Bellon, Steven F.;Booker, Shon K.;Cheng, Yuan;Coxon, Angela;Dominguez, Celia;Fellows, Ingrid;Hoffman, Douglas;Hungate, Randall;Kaplan-Lefko, Paula;Lee, Matthew R.;Li, Chun;Liu, Longbin;Rainbeau, Elizabeth;Reider, Paul J.;Rex, Karen;Siegm,期刊：Journal of Medicinal Chemistry, 页码：5766-5779 , 文章类型： 研究论文，,卷期：2008年51-18] C-Met is a receptor tyrosine kinase that plays a key role in several cellular processes but has also been found to be overexpressed and mutated in different human cancers. Consequently, targeting this enzyme has become ... Targeting the Ribose and Phosphate Binding Site of p38 Mitogen-Activated Protein (MAP) Kinase: Synthesis and Biological Testing of 2-Alkylsulfanyl-, 4(5)-Aryl-, 5(4)-Heteroaryl-Substituted Imidazoles. [作者：Koch, Pierre;Baeuerlein, Christiane;Jank, Hartmut;Laufer, Stefan;,期刊：Journal of Medicinal Chemistry, 页码：5630-5640 , 文章类型： 研究论文，,卷期：2008年51-18] (Heterocyclic Compounds (More Than One Hetero Atom)) Section Three series of substituted 2-alkylsulfanyl-4-(4-fluorophenyl)imidazoles, 5-pyridinyl-, 1-methyl-5-pyridinyl-, and 5-(2-aminopyridin-4-yl)-imidazoles, were pre... Discovery of Potent and Selective Small-Molecule PAR-2 Agonists. [作者：Seitzberg, Jimmi Gerner;Knapp, Anne Eeg;Lund, Birgitte Winther;Mandrup Bertozzi, Sine;Currier, Erika A.;Ma, Jian-Nong;Sherbukhin, Vladimir;Burstein, Ethan S.;Olsson, Roger;,期刊：Journal of Medicinal Chemistry, 页码：5490-5493 , 文章类型： 研究论文，,卷期：2008年51-18] conditions with a strong inflammatory component. We present the discovery and characterization of two structurally different, potent, selective, and metabolically stable small-mol. PAR-2 agonists. These ligands may be ... Structure-Guided Design of N-Phenyl Tertiary Amines as Transrepression-Selective Liver X Receptor Modulators with Anti-Inflammatory Activity. [作者：Chao, Esther Y.;Caravella, Justin A.;Watson, Mike A.;Campobasso, Nino;Ghisletti, Serena;Billin, Andrew N.;Galardi, Cristin;Wang, Ping;Laffitte, Bryan A.;Iannone, Marie A.;Goodwin, Bryan J.;Nichols, Jason A.;Parks, Derek J.;Stewart, Eugene;Wiethe, Robert W,期刊：Journal of Medicinal Chemistry, 页码：5758-5765 , 文章类型： 研究论文，,卷期：2008年51-18] A cocrystal structure of T1317 (3) bound to hLXRb was utilized in the design of a series of substituted N-Ph tertiary amines. Profiling in binding and functional assays led to the identification of LXR modulator GSK9772... Adamantyl-Substituted Retinoid-Derived Molecules That Interact with the Orphan Nuclear Receptor Small Heterodimer Partner: Effects of Replacing the 1-Adamantyl or Hydroxyl Group on Inhibition of Cancer Cell Growth, Induction of Cancer Cell Apoptosis, and [作者：Dawson, Marcia I.;Xia, Zebin;Jiang, Tao;Ye, Mao;Fontana, Joseph A.;Farhana, Lulu;Patel, Bhaumik;Xue, Li Ping;Bhuiyan, Mohammad;Pellicciari, Roberto;Macchiarulo, Antonio;Nuti, Roberto;Zhang, Xiao-Kun;Han, Young-Hoon;Tautz, Lutz;Hobbs, Peter D.;Jong, Ling;W,期刊：Journal of Medicinal Chemistry, 页码：5650-5662 , 文章类型： 研究论文，,卷期：2008年51-18] (E)-4-[3-(1-Adamantyl)-4'-hydroxyphenyl]-3-chlorocinnamic acid (3-Cl-AHPC) induces the cell-cycle arrest and apoptosis of leukemia and cancer cells. Studies demonstrated that 3-Cl-AHPC bound to the atypical orphan nucle... Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection. [作者：Summa, Vincenzo;Petrocchi, Alessia;Bonelli, Fabio;Crescenzi, Benedetta;Donghi, Monica;Ferrara, Marco;Fiore, Fabrizio;Gardelli, Cristina;Gonzalez Paz, Odalys;Hazuda, Daria J.;Jones, Philip;Kinzel, Olaf;Laufer, Ralph;Monteagudo, Edith;Muraglia, Ester;Nizi,,期刊：Journal of Medicinal Chemistry, 页码：5843-5855 , 文章类型： 研究论文，,卷期：2008年51-18] Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded enzymes required for replication and therefore a rational target for chemotherapeutic intervention in the treatment of HIV-1 infec... Synthesis, Ex Vivo Evaluation, and Radiolabeling of Potent 1,5-Diphenylpyrrolidin-2-one Cannabinoid Subtype-1 Receptor Ligands as Candidates for In Vivo Imaging. [作者：Donohue, Sean R.;Krushinski, Joseph H.;Pike, Victor W.;Chernet, Eyassu;Phebus, Lee;Chesterfield, Amy K.;Felder, Christian C.;Halldin, Christer;Schaus, John M.;,期刊：Journal of Medicinal Chemistry, 页码：5833-5842 , 文章类型： 研究论文，,卷期：2008年51-18] (Heterocyclic Compounds (One Hetero Atom)) Section We have reported that [methyl-11C] (3R,5R)-5-(3-methoxyphenyl)-3-[(R)-1-phenylethylamino]-1-(4-trifluorom ethylphenyl)pyrrolidin-2-one (I, R = OC11H3) binds with high se... Discovery and Labeling of High-Affinity 3,4-Diarylpyrazolines as Candidate Radioligands for In Vivo Imaging of Cannabinoid Subtype-1 (CB1) Receptors. [作者：Donohue, Sean R.;Pike, Victor W.;Finnema, Sjoerd J.;Truong, Phong;Andersson, Jan;Gulyas, Balazs;Halldin, Christer;,期刊：Journal of Medicinal Chemistry, 页码：5608-5616 , 文章类型： 研究论文，,卷期：2008年51-18] Imaging of cannabinoid subtype-1 (CB1) receptors in vivo with positron emission tomog. (PET) is likely to be important for understanding their role in neuropsychiatric disorders and for drug development. Radioligands for... Optimizing Natural Products by Biosynthetic Engineering: Discovery of Nonquinone Hsp90 Inhibitors. [作者：Zhang, Ming-Qiang;Gaisser, Sabine;Nur-E-Alam, Mohammad;Sheehan, Lesley S.;Vousden, William A.;Gaitatzis, Nikolaos;Peck, Gerrard;Coates, Nigel J.;Moss, Steven J.;Radzom, Markus;Foster, Teresa A.;Sheridan, Rose M.;Gregory, Matthew A.;Roe, S. Mark;Prodromou,,期刊：Journal of Medicinal Chemistry, 页码：5494-5497 , 文章类型： 研究论文，,卷期：2008年51-18] A biosynthetic medicinal chem. approach was applied to the optimization of the natural product Hsp90 inhibitor macbecin. By genetic engineering, mutants have been created to produce novel macbecin analogs including a no... Inactivation of NF-kB Components by Covalent Binding of (-)-Dehydroxymethylepoxyquinomicin to Specific Cysteine Residues. [作者：Yamamoto, Mizuki;Horie, Ryouichi;Takeiri, Masatoshi;Kozawa, Ikuko;Umezawa, Kazuo;,期刊：Journal of Medicinal Chemistry, 页码：5780-5788 , 文章类型： 研究论文，,卷期：2008年51-18] Previously, the authors designed and synthesized a potent NF-kB inhibitor, DHMEQ. Although DHMEQ showed potent anti-inflammatory and anticancer activities in animals, its mol. target has not been elucidated. In the pre... Inhibition of Geranylgeranyl Diphosphate Synthase by Bisphosphonates: A Crystallographic and Computational Investigation. [作者：Chen, Cammy K.-M.;Hudock, Michael P.;Zhang, Yonghui;Guo, Rey-Ting;Cao, Rong;No, Joo Hwan;Liang, Po-Huang;Ko, Tzu-Ping;Chang, Tao-Hsin;Chang, Shiou-chi;Song, Yongcheng;Axelson, Jordan;Kumar, Anup;Wang, Andrew H.-J.;Oldfield, Eric;,期刊：Journal of Medicinal Chemistry, 页码：5594-5607 , 文章类型： 研究论文，,卷期：2008年51-18] We report the X-ray structures of several bisphosphonate inhibitors of geranylgeranyl diphosphate synthase, a target for anticancer drugs. Bisphosphonates contg. unbranched side chains bind to either the farnesyl diphosp... Potent Cationic Inhibitors of West Nile Virus NS2B/NS3 Protease With Serum Stability, Cell Permeability and Antiviral Activity. [作者：Stoermer, Martin J.;Chappell, Keith J.;Liebscher, Susann;Jensen, Christina M.;Gan, Chun H.;Gupta, Praveer K.;Xu, Wei-Jun;Young, Paul R.;Fairlie, David P.;,期刊：Journal of Medicinal Chemistry, 页码：5714-5721 , 文章类型： 研究论文，,卷期：2008年51-18] West Nile virus (WNV) has spread rapidly around the globe, efficiently crossing species from migrating birds into humans and other mammals. The viral protease NS2B-NS3 is important for WNV replication and recognizes dib... Molecular Engineering of Conotoxins: The Importance of Loop Size to a-Conotoxin Structure and Function. [作者：Jin, Ai-Hua;Daly, Norelle L.;Nevin, Simon T.;Wang, Ching-I. A.;Dutertre, Sebastien;Lewis, Richard J.;Adams, David J.;Craik, David J.;Alewood, Paul F.;,期刊：Journal of Medicinal Chemistry, 页码：5575-5584 , 文章类型： 研究论文，,卷期：2008年51-18] a-Conotoxins are competitive antagonists of nicotinic acetylcholine receptors (nAChRs). The majority of currently characterized a-conotoxins have a 4/7 loop size, and the major features of neuronal a-conotoxins include ... Discovery of Novel and Cardioselective Diltiazem-like Calcium Channel Blockers via Virtual Screening. [作者：Carosati, Emanuele;Budriesi, Roberta;Ioan, Pierfranco;Ugenti, Maria P.;Frosini, Maria;Fusi, Fabio;Corda, Gaetano;Cosimelli, Barbara;Spinelli, Domenico;Chiarini, Alberto;Cruciani, Gabriele;,期刊：Journal of Medicinal Chemistry, 页码：5552-5565 , 文章类型： 研究论文，,卷期：2008年51-18] With the effort to discover new chemotypes blocking L-type calcium channels (LTCCs), ligand-based virtual screening was applied with a specific interest toward the diltiazem binding site. Roughly 50000 com. available co... Synthesis and Antitumor Activity of Mechercharmycin A Analogues. [作者：Hernandez, Delia;Altuna, Marta;Cuevas, Carmen;Aligue, Rosa;Albericio, Fernando;Alvarez, Mercedes;,期刊：Journal of Medicinal Chemistry, 页码：5722-5730 , 文章类型： 研究论文，,卷期：2008年51-18] such as I (R = H; R1 = H, MeOCH2CH2OCH2CH2OCH2COOCH2; RR1 = CH2) are prepd. as antitumor agents and tested for their inhibition of human cancer cell lines. Of the compds. tested, I (R = H; R1 = H, MeOCH2CH2OCH2CH2OCH2CO... Aminoacyl-anthraquinone conjugates as telomerase inhibitors: synthesis, biophysical and biological evaluation. [作者：Zagotto, Giuseppe;Sissi, Claudia;Lucatello, Lorena;Pivetta, Claudia;Cadamuro, Sergio A.;Fox, Keith R.;Neidle, Stephen;Palumbo, Manlio;,期刊：Journal of Medicinal Chemistry, 页码：5566-5574 , 文章类型： 研究论文，,卷期：2008年51-18] The telomerase-telomere complex is a prospective anticancer target. To inhibit enzyme activity by induction of G-quadruplex in human telomeres, we have synthesized a small library of 2,6- and 2,7-amino-acyl/peptidyl anth...