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2005
Enzyme inhibiting activity
X 0220
Discovery of Novel 2-(Aminoheteroaryl)-thiazole-5-carboxamides as Potent and
Active Src-Family Kinase p56Lck Inhibitors. — Optimization of the in vitro
15- 242 Orally
potency of a potent Lck inhibitor with modest cellular activity leads to the identification
of analogues with sub-nanomolar activities against Lck and single digit nanomolar inhibitory activities against T cell proliferation. Among them, compound (Ia) displays a
pharmacokinetic profile suitable for oral administration and excellent in vivo efficacy.
— (CHEN*, P.; et al.; Bioorg. Med. Chem. Lett. 14 (2004) 24, 6061-6066; Dep.
Discovery Chem., Bristol-Myers Squibb Pharm. Res. Inst., Princeton, NJ 08543, USA;
Eng.) — H. Hoennerscheid
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