title: Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
abstract: A series of substituted 2-(aminoheteroaryl)-thiazole-5-carboxamide analogs have been synthesized as novel, potent inhibitors of the Src-family kinase p56Lck. Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy.
authors.affiliation: Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. ping.chen@bms.com
authors.forename: Ping
authors.initials: P
authors.lastname: Chen
authors.forename: Derek
authors.initials: D
authors.lastname: Norris
authors.forename: Jagabandhu
authors.initials: J
authors.lastname: Das
authors.forename: Steven H
authors.initials: SH
authors.lastname: Spergel
authors.forename: John
authors.initials: J
authors.lastname: Wityak
authors.forename: Leslie
authors.initials: L
authors.lastname: Leith
authors.forename: Rulin
authors.initials: R
authors.lastname: Zhao
authors.forename: Bang-Chi
authors.initials: BC
authors.lastname: Chen
authors.forename: Sidney
authors.initials: S
authors.lastname: Pitt
authors.forename: Suhong
authors.initials: S
authors.lastname: Pang
authors.forename: Ding Ren
authors.initials: DR
authors.lastname: Shen
authors.forename: Rosemary
authors.initials: R
authors.lastname: Zhang
authors.forename: Henry F
authors.initials: HF
authors.lastname: De Fex
authors.forename: Arthur M
authors.initials: AM
authors.lastname: Doweyko
authors.forename: Kim W
authors.initials: KW
authors.lastname: McIntyre
authors.forename: David J
authors.initials: DJ
authors.lastname: Shuster
authors.forename: Kamelia
authors.initials: K
authors.lastname: Behnia
authors.forename: Gary L
authors.initials: GL
authors.lastname: Schieven
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish
mesh_terms: D000284:Administration, Oral; D000577:Amides / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D001169:Arthritis, Experimental / Q000628:therapy; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Q000037:antagonists & inhibitors*; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000577:Amides; D000893:Anti-Inflammatory Agents; D004791:Enzyme Inhibitors; D013844:Thiazoles; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck); D019061:src-Family Kinases