Discovery of a 1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity

被引:121
作者
Wittman, M
Carboni, J
Attar, R
Balasubramanian, B
Balimane, P
Brassil, P
Beaulieu, F
Chang, CY
Clarke, W
Dell, J
Eummer, J
Frennesson, D
Gottardis, M
Greer, A
Hansel, S
Hurlburt, W
Jacobson, B
Krishnananthan, S
Lee, FY
Li, AX
Lin, TA
Liu, PY
Ouellet, C
Sang, XP
Saulnier, MG
Stoffan, K
Sun, Y
Velaparthi, U
Wong, H
Yang, Z
Zimmermann, K
Zoeckler, M
Vyas, D
机构
[1] Bristol Myers Squibb Co, Discovey Chem, Wallingford, CT 06492 USA
[2] Bristol Myers Squibb Co, Dept Metab & Pharmacokinet, Wallingford, CT 06492 USA
[3] Bristol Myers Squibb Co, Dept Comp Aided Drug Design, Wallingford, CT 06492 USA
[4] Bristol Myers Squibb Co, Dept Chem Synth, Wallingford, CT 06492 USA
[5] Bristol Myers Squibb Co, Discovey Chem, Candiac, PQ, Canada
[6] Bristol Myers Squibb Co, Dept Oncol Drug Discovery, Princeton, NJ 08540 USA
[7] Bristol Myers Squibb Co, Dept Metab & Pharmacokinet, Princeton, NJ 08540 USA
[8] Bristol Myers Squibb Co, Dept Macromol Struct, Princeton, NJ 08540 USA
关键词
D O I
10.1021/jm050392q
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Compound 3 (BMS-536924), a novel small-molecule inhibitor of the insulin-like growth factor receptor kinase with equal potency against the insulin receptor is described. The in vitro and in vivo biological activity of this interesting compound is also reported.
引用
收藏
页码:5639 / 5643
页数:5
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