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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35条记录   A Small Molecule Inhibitor, 1,2,4,5-Benzenetetraamine Tetrahydrochloride, Targeting the Y397 Site of Focal Adhesion Kinase Decreases Tumor Growth. [作者：Golubovskaya, Vita M.;Nyberg, Carl;Zheng, Min;Kweh, Frederick;Magis, Andrew;Ostrov, David;Cance, William G.;,期刊：Journal of Medicinal Chemistry, 页码：7405-7416 , 文章类型： 研究论文，,卷期：2008年51-23] Focal adhesion kinase (FAK) is a nonreceptor kinase that is overexpressed in many types of tumors. We developed a novel cancer-therapy approach, targeting the main autophosphorylation site of FAK, Y397, by computer mode... Prolyl Oligopeptidase Inhibition by N-Acyl-pro-pyrrolidine-type Molecules. [作者：Kanai, Karoly;Aranyi, Peter;Bocskei, Zsolt;Ferenczy, Gyorgy;Harmat, Veronika;Simon, Kalman;Batori, Sandor;Naray-Szabo, Gabor;Hermecz, Istvan;,期刊：Journal of Medicinal Chemistry, 页码：7514-7522 , 文章类型： 研究论文，,卷期：2008年51-23] Three novel, N-acyl-pro-pyrrolidine-type, inhibitors of prolyl oligopeptidase (POP) with nanomolar activities were synthesized and their binding analyzed to the host enzyme in the light of X-ray diffraction and mol. mode... Synthesis and Structure-Activity Relationship Studies of 2-(N-Substituted)-aminobenzimidazoles as Potent Negative Gating Modulators of Small Conductance Ca2+-Activated K+ Channels. [作者：Sorensen, Ulrik S.;Strobaek, Dorte;Christophersen, Palle;Hougaard, Charlotte;Jensen, Marianne L.;Nielsen, Elsebet O.;Peters, Dan;Teuber, Lene;,期刊：Journal of Medicinal Chemistry, 页码：7625-7634 , 文章类型： 研究论文，,卷期：2008年51-23] Small conductance Ca2+-activated K+ channels (SK channels) participate in the control of neuronal excitability, in the shaping of action potential firing patterns, and in the regulation of synaptic transmission. SK chann... Histone Deacetylase Inhibitors through Click Chemistry. [作者：Shen, Jie;Woodward, Robert;Kedenburg, James Patrick;Liu, Xianwei;Chen, Min;Fang, Lanyan;Sun, Duxin;Wang, Peng George;,期刊：Journal of Medicinal Chemistry, 页码：7417-7427 , 文章类型： 研究论文，,卷期：2008年51-23] Histone deacetylase inhibitors (HDACi) are a relatively new class of chemotherapy agents. Herein, we report a click-chem. based approach to the synthesis of HDACi. Fourteen agents were synthesized from the combination ... Activation of p16 Gene Silenced by DNA Methylation in Cancer Cells by Phosphoramidate Derivatives of 2'-Deoxyzebularine. [作者：Yoo, Christine B.;Valente, Rocco;Congiatu, Costantino;Gavazza, Federica;Angel, Annette;Siddiqui, Maqbool A.;Jones, Peter A.;McGuigan, Christopher;Marquez, Victor E.;,期刊：Journal of Medicinal Chemistry, 页码：7593-7601 , 文章类型： 研究论文，,卷期：2008年51-23] We report herein the application of the phosphoramidate ProTide technol. to improve the metab. of the DNA methytransferase inhibitor, zebularine (Z). Zebularine is a riboside that must undergo a complex metabolic transf... Discovery of Begacestat, a Notch-1-Sparing g-Secretase Inhibitor for the Treatment of Alzheimer's Disease. [作者：Mayer, Scott C.;Kreft, Anthony F.;Harrison, Boyd;Abou-Gharbia, Magid;Antane, Madelene;Aschmies, Suzan;Atchison, Kevin;Chlenov, Michael;Cole, Derek C.;Comery, Thomas;Diamantidis, George;Ellingboe, John;Fan, Kristi;Galante, Rocco;Gonzales, Cathleen;Ho, Doug,期刊：Journal of Medicinal Chemistry, 页码：7348-7351 , 文章类型： 研究论文，,卷期：2008年51-23] SAR on HTS hits 1 and 2 led to the potent, Notch-1-sparing GSI 9, which lowered brain Ab in Tg2576 mice at 100 mg/kg po. Converting the metabolically labile Me groups in 9 to trifluoromethyl groups afforded the more sta... Assessment of Additive/Nonadditive Effects in Structure-Activity Relationships: Implications for Iterative Drug Design. [作者：Patel, Yogendra;Gillet, Valerie J.;Howe, Trevor;Pastor, Joaquin;Oyarzabal, Julen;Willett, Peter;,期刊：Journal of Medicinal Chemistry, 页码：7552-7562 , 文章类型： 研究论文，,卷期：2008年51-23] Free-Wilson (FW) anal. is common practice in medicinal chem. and is based on the assumption that the contributions to activity made by substituents at different substitution positions are additive. We analyze eight near... A Non-Cross-Linking Platinum-Acridine Agent with Potent Activity in Non-Small-Cell Lung Cancer. [作者：Ma, Zhidong;Choudhury, Jayati Roy;Wright, Marcus W.;Day, Cynthia S.;Saluta, Gilda;Kucera, Gregory L.;Bierbach, Ulrich;,期刊：Journal of Medicinal Chemistry, 页码：7574-7580 , 文章类型： 研究论文，,卷期：2008年51-23] The cytotoxic complex, [PtCl(Am)2(ACRAMTU)](NO3)2 (1) ((Am)2 = ethane-1,2-diamine, en; ACRAMTU = 1-[2-(acridin-9-ylamino)ethyl]-1,3-dimethylthiourea), is a dual platinating/intercalating DNA binder that, unlike clin. pla... Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]b enzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethyla mino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Huma [作者：Chen, Chen;Wu, Dongpei;Guo, Zhiqiang;Xie, Qiu;Reinhart, Greg J.;Madan, Ajay;Wen, Jenny;Chen, Takung;Huang, Charles Q.;Chen, Mi;Chen, Yongsheng;Tucci, Fabio C.;Rowbottom, Martin;Pontillo, Joseph;Zhu, Yun-Fei;Wade, Warren;Saunders, John;Bozigian, Haig;Strut,期刊：Journal of Medicinal Chemistry, 页码：7478-7485 , 文章类型： 研究论文，,卷期：2008年51-23] The discovery of novel uracil phenylethylamines bearing a butyric acid as potent human gonadotropin-releasing hormone receptor (hGnRH-R) antagonists is described. A major focus of this optimization was to improve the CY... Novel Naphthalene-N-sulfonyl-D-glutamic Acid Derivatives as Inhibitors of MurD, a Key Peptidoglycan Biosynthesis Enzyme. [作者：Humljan, Jan;Kotnik, Miha;Contreras-Martel, Carlos;Blanot, Didier;Urleb, Uros;Dessen, Andrea;Solmajer, Tom;Gobec, Stanislav;,期刊：Journal of Medicinal Chemistry, 页码：7486-7494 , 文章类型： 研究论文，,卷期：2008年51-23] Mur ligases have essential roles in the biosynthesis of peptidoglycan, and they represent attractive targets for the design of novel antibacterials. MurD (UDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase) is the second... Impact of Plasticity and Flexibility on Docking Results for Cytochrome P450 2D6: A Combined Approach of Molecular Dynamics and Ligand Docking. [作者：Hritz, Jozef;de Ruiter, Anita;Oostenbrink, Chris;,期刊：Journal of Medicinal Chemistry, 页码：7469-7477 , 文章类型： 研究论文，,卷期：2008年51-23] Cytochrome P450s (CYPs) exhibit a large plasticity and flexibility in the active site allowing for the binding of a large variety of substrates. The impact of plasticity and flexibility on ligand binding is investigated... Dihydrofuro[3,4-c]pyridinones as Inhibitors of the Cytolytic Effects of the Pore-Forming Glycoprotein Perforin. [作者：Lena, Gersande;Trapani, Joseph A.;Sutton, Vivien R.;Ciccone, Annette;Browne, Kylie A.;Smyth, Mark J.;Denny, William A.;Spicer, Julie A.;,期刊：Journal of Medicinal Chemistry, 页码：7614-7624 , 文章类型： 研究论文，,卷期：2008年51-23] Dihydrofuro[3,4-c]pyridinones are the first class of small mols. reported to inhibit the cytolytic effects of the lymphocyte toxin perforin. A lead structure was identified from a high throughput screen, and a series of... Novel Acetylcholine and Carbamoylcholine Analogues: Development of a Functionally Selective a4b2 Nicotinic Acetylcholine Receptor Agonist. [作者：Hansen, Camilla P.;Jensen, Anders A.;Christensen, Jeppe K.;Balle, Thomas;Liljefors, Tommy;Frolund, Bente;,期刊：Journal of Medicinal Chemistry, 页码：7380-7395 , 文章类型： 研究论文，,卷期：2008年51-23] A series of carbamoylcholine and acetylcholine analogs were synthesized and characterized pharmacol. at neuronal nicotinic acetylcholine receptors (nAChRs). Several of the compds. displayed low nanomolar binding affinit... Novel Multifunctional Acyloxyalkyl Ester Prodrugs of 5-Aminolevulinic Acid Display Improved Anticancer Activity Independent and Dependent on Photoactivation. [作者：Berkovitch, Gili;Doron, Dvir;Nudelman, Abraham;Malik, Zvi;Rephaeli, Ada;,期刊：Journal of Medicinal Chemistry, 页码：7356-7369 , 文章类型： 研究论文，,卷期：2008年51-23] Multifunctional acyloxyalkyl ester prodrugs of 5-aminolevulinic acid in cancer cell lines inhibited the proteasome and induced apoptosis and heme synthesis. The most potent prodrug was butyryloxymethyl 5-amino-4-oxopent... Selectivity and Mechanism of Action of a Growth Factor Receptor-Bound Protein 2 Src Homology 2 Domain Binding Antagonist. [作者：Giubellino, Alessio;Shi, Zhen-Dan;Miller Jenkins, Lisa M.;Worthy, Karen M.;Bindu, Lakshman K.;Athauda, Gagani;Peruzzi, Benedetta;Fisher, Robert J.;Appella, Ettore;Burke, Terrence R.;Bottaro, Donald P.;,期刊：Journal of Medicinal Chemistry, 页码：7459-7468 , 文章类型： 研究论文，,卷期：2008年51-23] factor receptor-bound protein 2 (Grb2) Src homol. 2 (SH2) domain binding (1) blocks growth factor stimulated motility, invasion, and angiogenesis in cultured cell models, as well as tumor metastasis in animals. To chara... Design, Structure-Activity Relationships, X-ray Crystal Structure, and Energetic Contributions of a Critical P1 Pharmacophore: 3-Chloroindole-7-yl-Based Factor Xa Inhibitors. [作者：Shi, Yan;Sitkoff, Doree;Zhang, Jing;Klei, Herbert E.;Kish, Kevin;Liu, Eddie C.-K.;Hartl, Karen S.;Seiler, Steve M.;Chang, Ming;Huang, Christine;Youssef, Sonia;Steinbacher, Thomas E.;Schumacher, William A.;Grazier, Nyeemah;Pudzianowski, Andrew;Apedo, Atsu;,期刊：Journal of Medicinal Chemistry, 页码：7541-7551 , 文章类型： 研究论文，,卷期：2008年51-23] established factor Xa inhibitor series. The indole group was designed to hydrogen-bond with the carbonyl of Gly218, while its 3-Me or 3-chloro substituent was intended to interact with Tyr228. These interactions were s...