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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36条记录   The Unusual Binding Mode of Cnicin to the Antibacterial Target Enzyme MurA Revealed by X-ray Crystallography. [作者：Steinbach, Anke;Scheidig, Axel J.;Klein, Christian D.;,期刊：Journal of Medicinal Chemistry, 页码：5143-5147 , 文章类型： 研究论文，,卷期：2008年51-16] in complex with its substrate UNAG and the sesquiterpene lactone cnicin, a potent inhibitor of the enzyme. The structure reveals that MurA has catalyzed the formation of a covalent adduct between cnicin and UNAG. This ... NMR Screening for Lead Compounds Using Tryptophan-Mutated Proteins. [作者：Rothweiler, Ulli;Czarna, Anna;Weber, Lutz;Popowicz, Grzegorz M.;Brongel, Kinga;Kowalska, Kaja;Orth, Michael;Stemmann, Olaf;Holak, Tad A.;,期刊：Journal of Medicinal Chemistry, 页码：5035-5042 , 文章类型： 研究论文，,卷期：2008年51-16] NMR-based drug screening methods provide the most reliable characterization of binding propensities of ligands to their target proteins. They are, however, one of the least effective methods in terms of the amt. of prot... Selective Structure-Based Virtual Screening for Full and Partial Agonists of the b2 Adrenergic Receptor. [作者：de Graaf, Chris;Rognan, Didier;,期刊：Journal of Medicinal Chemistry, 页码：4978-4985 , 文章类型： 研究论文，,卷期：2008年51-16] The recently solved high-resoln. X-ray structure of the b2 adrenergic receptor has been challenged for its ability to discriminate inverse agonists/antagonists from partial/full agonists. Whereas the X-ray structure of ... Inhibitors of Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (Shp2) Based on Oxindole Scaffolds. [作者：Lawrence, Harshani R.;Pireddu, Roberta;Chen, Liwei;Luo, Yunting;Sung, Shen-Shu;Szymanski, Ann Marie;Yip, M. L. Richard;Guida, Wayne C.;Sebti, Said M.;Wu, Jie;Lawrence, Nicholas J.;,期刊：Journal of Medicinal Chemistry, 页码：4948-4956 , 文章类型： 研究论文，,卷期：2008年51-16] Screening of the NCI diversity set of compds. has led to the identification of NSC-117199, which inhibits the protein tyrosine phosphatase (PTP) Shp2 with an IC50 of 47 mM. A focused library incorporating an isatin scaf... Further Studies on Lead Compounds Containing the Opioid Pharmacophore Dmt-Tic. [作者：Balboni, Gianfranco;Fiorini, Stella;Baldisserotto, Anna;Trapella, Claudio;Sasaki, Yusuke;Ambo, Akihiro;Marczak, Ewa D.;Lazarus, Lawrence H.;Salvadori, Severo;,期刊：Journal of Medicinal Chemistry, 页码：5109-5117 , 文章类型： 研究论文，,卷期：2008年51-16] agonists H-Dmt-Tic-Gly-NH-Ph and H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid (UFP-512) were evaluated for the influence of the substitution of Gly with aspartic acid, its chirality, and the importance of the -NH-Ph and N1H-Bid hydr... Ring Expanded Nucleoside Analogues Inhibit RNA Helicase and Intracellular Human Immunodeficiency Virus Type 1 Replication. [作者：Yedavalli, Venkat S. R. K.;Zhang, Ning;Cai, Hongyi;Zhang, Peng;Starost, Matthew F.;Hosmane, Ramachandra S.;Jeang, Kuan-Teh;,期刊：Journal of Medicinal Chemistry, 页码：5043-5051 , 文章类型： 研究论文，,卷期：2008年51-16] A series of ring expanded nucleoside (REN) analogs were synthesized and screened for inhibition of cellular RNA helicase activity and human immunodeficiency virus type 1 (HIV-1) replication. I and II were identified to ... Enhanced Antimalarial Activity of Novel Synthetic Aculeatin Derivatives. [作者：Peuchmaur, Marine;Saidani, Nadia;Botte, Cyrille;Marechal, Eric;Vial, Henri;Wong, Yung-Sing;,期刊：Journal of Medicinal Chemistry, 页码：4870-4873 , 文章类型： 研究论文，,卷期：2008年51-16] We report the design, synthesis, and in vitro evaluation of novel polyspirocyclic structures, e.g. I, inspired by the antimalarial natural products, the aculeatins. A divergent synthetic strategy was conceived for the p... Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries. [作者：Malakoutikhah, Morteza;Teixido, Meritxell;Giralt, Ernest;,期刊：Journal of Medicinal Chemistry, 页码：4881-4889 , 文章类型： 研究论文，,卷期：2008年51-16] Several peptide families contg. N-methylated amino acids were designed and synthesized using solid-phase peptide synthesis (SPPS). The permeability and phospholipophilicity of these compds. were studied by parallel arti... Structure-Activity Relationship of Kahalalide F Synthetic Analogues. [作者：Jimenez, Jose C.;Lopez-Macia, Angel;Gracia, Carol;Varon, Sonia;Carrascal, Marta;Caba, Josep M.;Royo, Miriam;Francesch, Andres M.;Cuevas, Carmen;Giralt, Ernest;Albericio, Fernando;,期刊：Journal of Medicinal Chemistry, 页码：4920-4931 , 文章类型： 研究论文，,卷期：2008年51-16] Kahalalide F (KF) is a natural product currently under phase II clin. trials. Here, the authors report the solid-phase synthesis of 132 novel analogs of kahalalide F and their in vitro activity on a panel of up to 14 ca... Synthesis and Discovery of High Affinity Folate Receptor-Specific Glycinamide Ribonucleotide Formyltransferase Inhibitors with Antitumor Activity. [作者：Deng, Yijun;Wang, Yiqiang;Cherian, Christina;Hou, Zhanjun;Buck, Steven A.;Matherly, Larry H.;Gangjee, Aleem;,期刊：Journal of Medicinal Chemistry, 页码：5052-5063 , 文章类型： 研究论文，,卷期：2008年51-16] 6-Substituted classical pyrrolo[2,3-d]pyrimidine antifolates I (n = 4-6) with a three- to six-carbon bridge between the heterocycle and the benzoyl-L-glutamate were synthesized starting from Me 4-formylbenzoate and a Wit... Synthesis, Biological Evaluation, and Molecular Modeling of Abiraterone Analogues: Novel CYP17 Inhibitors for the Treatment of Prostate Cancer. [作者：Pinto-Bazurco Mendieta, Mariano A. E.;Negri, Matthias;Jagusch, Carsten;Mueller-Vieira, Ursula;Lauterbach, Thomas;Hartmann, Rolf W.;,期刊：Journal of Medicinal Chemistry, 页码：5009-5018 , 文章类型： 研究论文，,卷期：2008年51-16] 17a-hydroxylase-17,20-lyase inhibitor (CYP17), is currently undergoing phase II clin. trials as a potential drug for the treatment of androgen-dependent prostate cancer. Since steroidal compds. often show side effects a... Novel 1,4-Benzothiazine Derivatives as Large Conductance Ca2+-Activated Potassium Channel Openers. [作者：Calderone, Vincenzo;Spogli, Roberto;Martelli, Alma;Manfroni, Giuseppe;Testai, Lara;Sabatini, Stefano;Tabarrini, Oriana;Cecchetti, Violetta;,期刊：Journal of Medicinal Chemistry, 页码：5085-5092 , 文章类型： 研究论文，,卷期：2008年51-16] The design and synthesis of a novel class of 1,4-benzothiazines, e.g. I, targeted for the large-conductance calcium-activated potassium channels (BK) are presented. In vitro functional characterization of BK channel ope... Sulindac Derivatives That Activate the Peroxisome Proliferator-activated Receptor g but Lack Cyclooxygenase Inhibition. [作者：Felts, Andrew S.;Siegel, Brianna S.;Young, Shiu M.;Moth, Christopher W.;Lybrand, Terry P.;Dannenberg, Andrew J.;Marnett, Lawrence J.;Subbaramaiah, Kotha;,期刊：Journal of Medicinal Chemistry, 页码：4911-4919 , 文章类型： 研究论文，,卷期：2008年51-16] A series of novel derivs. of the nonsteroidal anti-inflammatory drug (NSAID) sulindac sulfide, e.g. I (R = C6H4SMe, C6H4CF3, 8-quinolinyl, etc.), were synthesized as potential agonists of the peroxisome proliferator-acti... Exploiting Ordered Waters in Molecular Docking. [作者：Huang, Niu;Shoichet, Brian K.;,期刊：Journal of Medicinal Chemistry, 页码：4862-4865 , 文章类型： 研究论文，,卷期：2008年51-16] protein-ligand interactions. The authors explore switching ordered water mols. "on" and "off" during docking screens of a large library. The method assumes additivity and scales linearly with the no. of waters sampled d... Design and Synthesis of a Novel Series of N-Alkyl Isatin Acylhydrazone Derivatives that Act as Selective Cannabinoid Receptor 2 Agonists for the Treatment of Neuropathic Pain. [作者：Diaz, Philippe;Xu, Jijun;Astruc-Diaz, Fanny;Pan, Hao-Min;Brown, David L.;Naguib, Mohamed;,期刊：Journal of Medicinal Chemistry, 页码：4932-4947 , 文章类型： 研究论文，,卷期：2008年51-16] There is growing interest in using cannabinoid receptor 2 (CB2) agonists for the treatment of neuropathic pain. We have synthesized a novel series of N-alkyl isatin acylhydrazone derivs., e.g. I (R1 = 1-pentyl, Ph, PhCH... Blockade of Glucocorticoid Excess at the Tissue Level: Inhibitors of 11b-Hydroxysteroid Dehydrogenase Type 1 as a Therapy for Type 2 Diabetes. [作者：Fotsch, Christopher;Wang, Minghan;,期刊：Journal of Medicinal Chemistry, 页码：4851-4857 , 文章类型： 综述，,卷期：2008年51-16] A review.