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Overcoming the genotoxicity of a pyrrolidine substituted arylindenopyrimidine as a potent dual adenosine A(2A)/A(1) antagonist by minimizing bioactivation to an iminium ion reactive intermediate.
Lim HK, Chen J, Sensenhauser C, Cook K, Preston R, Thomas T, Shook B, Jackson PF, Rassnick S, Rhodes K, Gopaul V, Salter R, Silva J, Evans DC. Lim HK, et al. Among authors: evans dc. Chem Res Toxicol. 2011 Jul 18;24(7):1012-30. doi: 10.1021/tx1004437. Epub 2011 Jun 28. Chem Res Toxicol. 2011. PMID: 21667953
Evidence for the bioactivation of zomepirac and tolmetin by an oxidative pathway: identification of glutathione adducts in vitro in human liver microsomes and in vivo in rats.
Chen Q, Doss GA, Tung EC, Liu W, Tang YS, Braun MP, Didolkar V, Strauss JR, Wang RW, Stearns RA, Evans DC, Baillie TA, Tang W. Chen Q, et al. Among authors: evans dc. Drug Metab Dispos. 2006 Jan;34(1):145-51. doi: 10.1124/dmd.105.004341. Epub 2005 Oct 26. Drug Metab Dispos. 2006. PMID: 16251255
In vitro bioactivation of dihydrobenzoxathiin selective estrogen receptor modulators by cytochrome P450 3A4 in human liver microsomes: formation of reactive iminium and quinone type metabolites.
Zhang Z, Chen Q, Li Y, Doss GA, Dean BJ, Ngui JS, Silva Elipe M, Kim S, Wu JY, Dininno F, Hammond ML, Stearns RA, Evans DC, Baillie TA, Tang W. Zhang Z, et al. Among authors: evans dc. Chem Res Toxicol. 2005 Apr;18(4):675-85. doi: 10.1021/tx0496789. Chem Res Toxicol. 2005. PMID: 15833027
Identification of potential pharmacological and toxicological targets differentiating structural analogs by a combination of transcriptional profiling and promoter analysis in LS-180 and Caco-2 adenocarcinoma cell lines.
Hartley DP, Dai X, Yabut J, Chu X, Cheng O, Zhang T, He YD, Roberts C, Ulrich R, Evers R, Evans DC. Hartley DP, et al. Among authors: evans dc. Pharmacogenet Genomics. 2006 Aug;16(8):579-99. doi: 10.1097/01.fpc.0000220561.59972.7a. Pharmacogenet Genomics. 2006. PMID: 16847427
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