Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56Lck

被引：43

作者：

Chen, P

Norris, D

Iwanowicz, EJ

Spergel, SH

Lin, J

Gu, HH

Shen, ZQ

Wityak, J

Lin, TA

Pang, SH

De Fex, HF

Pitt, S

Shen, DR

Doweyko, AM

Bassolino, DA

Roberge, JY

Poss, MA

Chen, BC

Schieven, GL

Barrish, JC

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Discovery Chem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Early Discovery Chem, Princeton, NJ 08543 USA

[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Comp Aided Drug Design, Princeton, NJ 08543 USA

[4] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Immunol Inflammat & Pulm Drug Discovery, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(02)00191-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have identified a novel series of 1,5-imidizoquinoxalines as inhibitors of Lck with excellent potency (IC(50)s less than or equal to 5 nM) as well as good cellular activity against T-cell proliferation (IC(50)s < 1 muM). Structure-activity studies demonstrate the requirement for the core heterocycle in addition to an optimal 2.6-disubstituted aniline group. (C) 2002 Published by Elsevier Science Ltd.

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页码：1361 / 1364

页数：4

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