100 related articles for article (PubMed ID: 18227141)
1. Metabolite generation via microbial biotransformations with Actinomycetes: rapid screening for active strains and biosynthesis of important human metabolites of two development-stage compounds, 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101) and dasatinib.
Li W; Josephs JL; Skiles GL; Humphreys WG
Drug Metab Dispos; 2008 Apr; 36(4):721-30. PubMed ID: 18227141
[TBL] [Abstract][Full Text] [Related]
2. Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.
Potin D; Launay M; Monatlik F; Malabre P; Fabreguettes M; Fouquet A; Maillet M; Nicolai E; Dorgeret L; Chevallier F; Besse D; Dufort M; Caussade F; Ahmad SZ; Stetsko DK; Skala S; Davis PM; Balimane P; Patel K; Yang Z; Marathe P; Postelneck J; Townsend RM; Goldfarb V; Sheriff S; Einspahr H; Kish K; Malley MF; DiMarco JD; Gougoutas JZ; Kadiyala P; Cheney DL; Tejwani RW; Murphy DK; Mcintyre KW; Yang X; Chao S; Leith L; Xiao Z; Mathur A; Chen BC; Wu DR; Traeger SC; McKinnon M; Barrish JC; Robl JA; Iwanowicz EJ; Suchard SJ; Dhar TG
J Med Chem; 2006 Nov; 49(24):6946-9. PubMed ID: 17125246
[TBL] [Abstract][Full Text] [Related]
3. Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics.
Wang L; Christopher LJ; Cui D; Li W; Iyer R; Humphreys WG; Zhang D
Drug Metab Dispos; 2008 Sep; 36(9):1828-39. PubMed ID: 18556438
[TBL] [Abstract][Full Text] [Related]
4. 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
Das J; Chen P; Norris D; Padmanabha R; Lin J; Moquin RV; Shen Z; Cook LS; Doweyko AM; Pitt S; Pang S; Shen DR; Fang Q; de Fex HF; McIntyre KW; Shuster DJ; Gillooly KM; Behnia K; Schieven GL; Wityak J; Barrish JC
J Med Chem; 2006 Nov; 49(23):6819-32. PubMed ID: 17154512
[TBL] [Abstract][Full Text] [Related]
5. Metabolism of an atypical antipsychotic agent, 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2, 5,5-trimethyl-4-thiazolidinone (HP236).
Mutlib AE; Jurcak J; Hrib N
Drug Metab Dispos; 1996 Oct; 24(10):1139-50. PubMed ID: 8894517
[TBL] [Abstract][Full Text] [Related]
6. Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).
Watterson SH; Xiao Z; Dodd DS; Tortolani DR; Vaccaro W; Potin D; Launay M; Stetsko DK; Skala S; Davis PM; Lee D; Yang X; McIntyre KW; Balimane P; Patel K; Yang Z; Marathe P; Kadiyala P; Tebben AJ; Sheriff S; Chang CY; Ziemba T; Zhang H; Chen BC; DelMonte AJ; Aranibar N; McKinnon M; Barrish JC; Suchard SJ; Murali Dhar TG
J Med Chem; 2010 May; 53(9):3814-30. PubMed ID: 20405922
[TBL] [Abstract][Full Text] [Related]
7. Characterization of in vitro metabolites of trimethoprim and diaveridine in pig liver microsomes by liquid chromatography combined with hybrid ion trap/time-of-flight mass spectrometry.
Liu ZY; Wu Y; Sun ZL; Wan L
Biomed Chromatogr; 2012 Sep; 26(9):1101-8. PubMed ID: 22161732
[TBL] [Abstract][Full Text] [Related]
8. Biotransformation of [14C]dasatinib: in vitro studies in rat, monkey, and human and disposition after administration to rats and monkeys.
Christopher LJ; Cui D; Li W; Barros A; Arora VK; Zhang H; Wang L; Zhang D; Manning JA; He K; Fletcher AM; Ogan M; Lago M; Bonacorsi SJ; Humphreys WG; Iyer RA
Drug Metab Dispos; 2008 Jul; 36(7):1341-56. PubMed ID: 18420785
[TBL] [Abstract][Full Text] [Related]
9. A validated LC-MS/MS assay for the simultaneous determination of the anti-leukemic agent dasatinib and two pharmacologically active metabolites in human plasma: application to a clinical pharmacokinetic study.
Furlong MT; Agrawal S; Hawthorne D; Lago M; Unger S; Krueger L; Stouffer B
J Pharm Biomed Anal; 2012 Jan; 58():130-5. PubMed ID: 21982905
[TBL] [Abstract][Full Text] [Related]
10. A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif.
Kalgutkar AS; Driscoll J; Zhao SX; Walker GS; Shepard RM; Soglia JR; Atherton J; Yu L; Mutlib AE; Munchhof MJ; Reiter LA; Jones CS; Doty JL; Trevena KA; Shaffer CL; Ripp SL
Chem Res Toxicol; 2007 Dec; 20(12):1954-65. PubMed ID: 17935300
[TBL] [Abstract][Full Text] [Related]
11. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Lombardo LJ; Lee FY; Chen P; Norris D; Barrish JC; Behnia K; Castaneda S; Cornelius LA; Das J; Doweyko AM; Fairchild C; Hunt JT; Inigo I; Johnston K; Kamath A; Kan D; Klei H; Marathe P; Pang S; Peterson R; Pitt S; Schieven GL; Schmidt RJ; Tokarski J; Wen ML; Wityak J; Borzilleri RM
J Med Chem; 2004 Dec; 47(27):6658-61. PubMed ID: 15615512
[TBL] [Abstract][Full Text] [Related]
12. Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL.
Kamath AV; Wang J; Lee FY; Marathe PH
Cancer Chemother Pharmacol; 2008 Mar; 61(3):365-76. PubMed ID: 17429625
[TBL] [Abstract][Full Text] [Related]
13. Metabolism and disposition of dasatinib after oral administration to humans.
Christopher LJ; Cui D; Wu C; Luo R; Manning JA; Bonacorsi SJ; Lago M; Allentoff A; Lee FY; McCann B; Galbraith S; Reitberg DP; He K; Barros A; Blackwood-Chirchir A; Humphreys WG; Iyer RA
Drug Metab Dispos; 2008 Jul; 36(7):1357-64. PubMed ID: 18420784
[TBL] [Abstract][Full Text] [Related]
14. Synthesis and biological activities of 2-amino-thiazole-5-carboxylic acid phenylamide derivatives.
Liu W; Zhou J; Qi F; Bensdorf K; Li Z; Zhang H; Qian H; Huang W; Cai X; Cao P; Wellner A; Gust R
Arch Pharm (Weinheim); 2011 Jul; 344(7):451-8. PubMed ID: 21598297
[TBL] [Abstract][Full Text] [Related]
15. Metabolism of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): identification of an unusual N-acetylglucosamine conjugate in the cynomolgus monkey.
Johnson BM; Kamath AV; Leet JE; Liu X; Bhide RS; Tejwani RW; Zhang Y; Qian L; Wei DD; Lombardo LJ; Shu YZ
Drug Metab Dispos; 2008 Dec; 36(12):2475-83. PubMed ID: 18787055
[TBL] [Abstract][Full Text] [Related]
16. Lacteal secretion, fetal and maternal tissue distribution of dasatinib in rats.
He K; Lago MW; Iyer RA; Shyu WC; Humphreys WG; Christopher LJ
Drug Metab Dispos; 2008 Dec; 36(12):2564-70. PubMed ID: 18787054
[TBL] [Abstract][Full Text] [Related]
17. Metabolism of the polynuclear sulfur heterocycle benzo[b]phenanthro[2,3-d]thiophene by rodent liver microsomes: evidence for multiple pathways in the bioactivation of benzo[b]phenanthro[2,3-d]thiophene.
Yuan ZX; Sikka HC; Munir S; Kumar A; Muruganandam AV; Kumar S
Chem Res Toxicol; 2003 Dec; 16(12):1581-8. PubMed ID: 14680372
[TBL] [Abstract][Full Text] [Related]
18. Inhibitory effect of paraquat on biotransformation of halothane in rabbit liver microsomes.
Kawamoto M; Fujii K; Yuge O; Morio M
Hiroshima J Med Sci; 1989 Dec; 38(4):161-7. PubMed ID: 2637243
[TBL] [Abstract][Full Text] [Related]
19. Bioactivation of isothiazoles: minimizing the risk of potential toxicity in drug discovery.
Teffera Y; Choquette D; Liu J; Colletti AE; Hollis LS; Lin MH; Zhao Z
Chem Res Toxicol; 2010 Nov; 23(11):1743-52. PubMed ID: 20825217
[TBL] [Abstract][Full Text] [Related]
20. CYP1A2-mediated biotransformation of cardioactive 2-thienylidene-3,4-methylenedioxybenzoylhydrazine (LASSBio-294) by rat liver microsomes and human recombinant CYP enzymes.
Fraga AG; da Silva LL; Fraga CA; Barreiro EJ
Eur J Med Chem; 2011 Jan; 46(1):349-55. PubMed ID: 21144625
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
