化学
铅化合物
组合化学
激酶
结构-活动关系
化学合成
立体化学
生物化学
体外
计算生物学
生物
作者
Roger A. Smith,James A. Barbosa,Cheri L. Blum,Mark A. Bobko,Yolanda Caringal,Robert Dally,Jeffrey S. Johnson,Michael E. Katz,Nancy Kennure,Jill Kingery-Wood,Wendy Lee,Timothy B. Lowinger,John F. Lyons,Vivienne Marsh,Daniel H. Rogers,Stephen G. Swartz,Tracy L. Walling,Hanno Wild
标识
DOI:10.1016/s0960-894x(01)00571-6
摘要
Heterocyclic ureas, such as N-3-thienyl N'-aryl ureas, have been identified as novel inhibitors of raf kinase, a key mediator in the ras signal transduction pathway. Structure-activity relationships were established, and the potency of the screening hit was improved 10-fold to IC(50)=1.7 microM. A combinatorial synthesis approach enabled the identification of a breakthrough lead (IC(50)=0.54 microM) for a second generation series of heterocyclic urea raf kinase inhibitors.
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