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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33条记录   Influence of Amphiphilic Block Copolymer Induced Changes in Membrane Ion Conductance on the Reversal of Multidrug Resistance. [作者：Sommer, Klaus;Kaiser, Sergej;Krylova, Oxana O.;Kressler, Joerg;Pohl, Peter;Busse, Karsten;,期刊：Journal of Medicinal Chemistry, 页码：4253-4259 , 文章类型： 研究论文，,卷期：2008年51-14] Block copolymers are able to reverse multidrug resistance (MDR) of tumor cells by a yet unknown mechanism. The drug efflux system's interactions or ATP depletion, resp., may be involved in MDR reversal as well as damage... Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target. [作者：Friesen, Richard W.;Mancini, Joseph A.;,期刊：Journal of Medicinal Chemistry, 页码：4059-4067 , 文章类型： 综述，,卷期：2008年51-14] A review. The use of NSAIDs (nonselective inhibitors of COX-1 and COX-2) and coxibs (selective inhibitors of COX-2) is a mainstay of anti-inflammatory and analgesic therapy. Since coxibs and NSAIDs intervene in the pro... Determination of the Microscopic Equilibrium Dissociation Constants for Risedronate and Its Analogues Reveals Two Distinct Roles for the Nitrogen Atom in Nitrogen-Containing Bisphosphonate Drugs. [作者：Hounslow, Andrea M.;Carran, John;Brown, Richard J.;Rejman, Dominik;Blackburn, G. Michael;Watts, Donald J.;,期刊：Journal of Medicinal Chemistry, 页码：4170-4178 , 文章类型： 研究论文，,卷期：2008年51-14] Microscopic equil. dissocn. consts., kas, were detd. for four nitrogen-contg. bisphosphonates (N-BP): risedronate and its analogs 2-(2-aminophenyl)-1-hydroxyethylidene-1,1-bisphosphonate, NE 11807, and NE 97220. The pro... Identification of a Potent, Selective, and Orally Active Leukotriene A4 Hydrolase Inhibitor with Anti-Inflammatory Activity. [作者：Grice, Cheryl A.;Tays, Kevin L.;Savall, Brad M.;Wei, Jianmei;Butler, Christopher R.;Axe, Frank U.;Bembenek, Scott D.;Fourie, Anne M.;Dunford, Paul J.;Lundeen, Katherine;Coles, Fawn;Xue, Xiaohua;Riley, Jason P.;Williams, Kacy N.;Karlsson, Lars;Edwards, Jam,期刊：Journal of Medicinal Chemistry, 页码：4150-4169 , 文章类型： 研究论文，,卷期：2008年51-14] enzyme with both hydrolase and aminopeptidase activity. As a hydrolase, LTA4H stereospecifically catalyzes the transformation of the unstable epoxide LTA4 to the diol LTB4, a potent chemoattractant and activator of neut... Tripod-like Cationic Lipids as Novel Gene Carriers. [作者：Unciti-Broceta, Asier;Holder, Emma;Jones, Lisa J.;Stevenson, Barbara;Turner, Andrew R.;Porteous, David J.;Boyd, A. Chris;Bradley, Mark;,期刊：Journal of Medicinal Chemistry, 页码：4076-4084 , 文章类型： 研究论文，,卷期：2008年51-14] An innovative family of tridentate-cationic single-chained lipids designed to enhance DNA compaction and to promote endosomal escape was synthesized by coupling various lipids to a multibranched scaffold. DNA retardatio... Ribose-Modified Purine Nucleosides as Ribonucleotide Reductase Inhibitors. Synthesis, Antitumor Activity, and Molecular Modeling of N6-Substituted 3'-C-Methyladenosine Derivatives. [作者：Cappellacci, Loredana;Franchetti, Palmarisa;Vita, Patrizia;Petrelli, Riccardo;Lavecchia, Antonio;Jayaram, Hiremagalur N.;Saiko, Philipp;Graser, Geraldine;Szekeres, Thomas;Grifantini, Mario;,期刊：Journal of Medicinal Chemistry, 页码：4260-4269 , 文章类型： 研究论文，,卷期：2008年51-14] A series of cycloalkyl, bicycloalkyl, aryl, and heteroaryl N6-substituted derivs. of the antitumor agent 3'-C-methyladenosine (3'-Me-Ado), an inhibitor of the a Rnr1 subunit of mammalian ribonucleotide reductase (RR), we... a2-Adrenoreceptors Profile Modulation. 4. From Antagonist to Agonist Behavior. [作者：Gentili, Francesco;Cardinaletti, Claudia;Vesprini, Cristian;Carrieri, Antonio;Ghelfi, Francesca;Farande, Aniket;Giannella, Mario;Piergentili, Alessandro;Quaglia, Wilma;Laurila, Jonne M.;Huhtinen, Anna;Scheinin, Mika;Pigini, Maria;,期刊：Journal of Medicinal Chemistry, 页码：4289-4299 , 文章类型： 研究论文，,卷期：2008年51-14] The goal of the present study was to modulate the receptor interaction properties of known a2-adrenoreceptor (AR) antagonists to obtain novel a2-AR agonists with desirable subtype selectivity. Therefore, a Ph group or o... SAR, Pharmacokinetics, Safety, and Efficacy of Glucokinase Activating 2-(4-Sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. [作者：Bertram, Lisa S.;Black, Daniel;Briner, Paul H.;Chatfield, Rosemary;Cooke, Andrew;Fyfe, Matthew C. T.;Murray, P. John;Naud, Frederic;Nawano, Masao;Procter, Martin J.;Rakipovski, Gunaj;Rasamison, Chrystelle M.;Reynet, Christine;Schofield, Karen L.;Shah, Vil,期刊：Journal of Medicinal Chemistry, 页码：4340-4345 , 文章类型： 研究论文，,卷期：2008年51-14] Allosteric activators of the glucose-sensing enzyme glucokinase (GK) are currently attracting much interest as potential antidiabetic therapies because they can achieve powerful blood glucose lowering through actions in ... Discovery of N-(2-Aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzam ide (MGCD0103), an Orally Active Histone Deacetylase Inhibitor. [作者：Zhou, Nancy;Moradei, Oscar;Raeppel, Stephane;Leit, Silvana;Frechette, Sylvie;Gaudette, Frederic;Paquin, Isabelle;Bernstein, Naomy;Bouchain, Giliane;Vaisburg, Arkadii;Jin, Zhiyun;Gillespie, Jeff;Wang, James;Fournel, Marielle;Yan, Pu T.;Trachy-Bourget, Mari,期刊：Journal of Medicinal Chemistry, 页码：4072-4075 , 文章类型： 研究论文，,卷期：2008年51-14] The design, synthesis, and biol. evaluation of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzam ide (MGCD0103) (I) is described. Compd. I is an isotype-selective small mol. histone deacetylase (HDAC... Chiral Aromatase and Dual Aromatase-Steroid Sulfatase Inhibitors from the Letrozole Template: Synthesis, Absolute Configuration, and In Vitro Activity. [作者：Wood, Paul M.;Woo, L. W. Lawrence;Labrosse, Jean-Robert;Trusselle, Melanie N.;Abbate, Sergio;Longhi, Giovanna;Castiglioni, Ettore;Lebon, France;Purohit, Atul;Reed, Michael J.;Potter, Barry V. L.;,期刊：Journal of Medicinal Chemistry, 页码：4226-4238 , 文章类型： 研究论文，,卷期：2008年51-14] Compounds (More Than One Hetero Atom)) Section To explore aromatase inhibition and to broaden the structural diversity of dual aromatase-sulfatase inhibitors (DASIs), the steroid sulfatase (STS) inhibitory pharmacophore ... Piperazine Sulfonamides as Potent, Selective, and Orally Available 11b-Hydroxysteroid Dehydrogenase Type 1 Inhibitors with Efficacy in the Rat Cortisone-Induced Hyperinsulinemia Model. [作者：Xiang, Jason;Wan, Zhao-Kui;Li, Huan-Qiu;Ipek, Manus;Binnun, Eva;Nunez, Jill;Chen, Lihren;McKew, John C.;Mansour, Tarek S.;Xu, Xin;Suri, Vipin;Tam, May;Xing, Yuzhe;Li, Xiangping;Hahm, Seung;Tobin, James;Saiah, Eddine;,期刊：Journal of Medicinal Chemistry, 页码：4068-4071 , 文章类型： 研究论文，,卷期：2008年51-14] 11b-Hydroxysteroid dehydrogenase type 1 (11b-HSD1) is the enzyme that converts cortisone to cortisol. Evidence suggests that selective inhibition of 11b-HSD1 could treat diabetes and metabolic syndrome. Presented herein... From Phenothiazine to 3-Phenyl-1,4-benzothiazine Derivatives as Inhibitors of the Staphylococcus aureus NorA Multidrug Efflux Pump. [作者：Sabatini, Stefano;Kaatz, Glenn W.;Rossolini, Gian Maria;Brandini, David;Fravolini, Arnaldo;,期刊：Journal of Medicinal Chemistry, 页码：4321-4330 , 文章类型： 研究论文，,卷期：2008年51-14] Overexpression of efflux pumps is an important mechanism by which bacteria evade effects of substrate antimicrobial agents and inhibition of such pumps is a promising strategy to circumvent this resistance mechanism. No... Design, Synthesis, and Biological Evaluation of Novel Tri- and Tetrasubstituted Imidazoles as Highly Potent and Specific ATP-Mimetic Inhibitors of p38 MAP Kinase: Focus on Optimized Interactions with the Enzyme's Surface-Exposed Front Region. [作者：Laufer, Stefan A.;Hauser, Dominik R. J.;Domeyer, David M.;Kinkel, Katrin;Liedtke, Andy J.;,期刊：Journal of Medicinal Chemistry, 页码：4122-4149 , 文章类型： 研究论文，,卷期：2008年51-14] The synthesis, biol. testing, and SAR of novel 2,4,5- and 1,2,4,5-substituted 2-thioimidazoles, e.g., I are described. Amino, oxy, or thioxy substituents at the 2-position of the pyridinyl moiety were evaluated for thei... Discovery of 4-Amino and 4-Hydroxy-1-aroylindoles as Potent Tubulin Polymerization Inhibitors. [作者：Liou, Jing-Ping;Wu, Zi-Yi;Kuo, Ching-Chuan;Chang, Chi-Yen;Lu, Pei-Yi;Chen, Chi-Ming;Hsieh, Hsing-Pang;Chang, Jang-Yang;,期刊：Journal of Medicinal Chemistry, 页码：4351-4355 , 文章类型： 研究论文，,卷期：2008年51-14] 1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivs., e.g., I and II, were synthesized and evaluated for anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles I and II, with IC50 of 0.... Potency and selectivity of trifluoroacetylimino and pyrazinoylimino nicotinic insecticides and their fit at a unique binding site niche. [作者：Tomizawa, Motohiro;Kagabu, Shinzo;Ohno, Ikuya;Durkin, Kathleen A.;Casida, John E.;,期刊：Journal of Medicinal Chemistry, 页码：4213-4218 , 文章类型： 研究论文，,卷期：2008年51-14] Neonicotinoid agonists with a nitroimino or cyanoimino pharmacophore are the newest of the four most important classes of insecticides. Studies on the nicotinic receptor structure in the neonicotinoid-bound state reveale... Carbamates with Differential Mechanism of Inhibition Toward Acetylcholinesterase and Butyrylcholinesterase. [作者：Darvesh, Sultan;Darvesh, Katherine V.;McDonald, Robert S.;Mataija, Diane;Walsh, Ryan;Mothana, Sam;Lockridge, Oksana;Martin, Earl;,期刊：Journal of Medicinal Chemistry, 页码：4200-4212 , 文章类型： 研究论文，,卷期：2008年51-14] Most carbamates are pseudoirreversible inhibitors of cholinesterases. Phenothiazine carbamates exhibit this inhibition of acetylcholinesterase but produce reversible inhibition of butyrylcholinesterase, suggesting that t...