- 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...
- 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....
- 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...
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