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The discovery of potent cRaf1 kinase inhibitors

✍ Scribed by Karen Lackey; Michael Cory; Ronda Davis; Stephen V. Frye; Philip A. Harris; Robert N. Hunter; David K. Jung; O.Bradley McDonald; Robert W. McNutt; Michael R. Peel; Randy D. Rutkowske; James M. Veal; Edgar R. Wood

Publisher
Elsevier Science
Year
2000
Tongue
English
Weight
168 KB
Volume
10
Category
Article
ISSN
0960-894X

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✦ Synopsis

A series of benzylidene-1H-indol-2-one (oxindole) derivatives was synthesized and evaluated as cRaf-1 kinase inhibitors. The key features of the molecules were the donor/acceptor motif common to kinase inhibitors and a critical acidic phenol flanked by two substitutions. Diverse 5-position substitutions provided compounds with low nanomolar kinase enzyme inhibition and inhibited the intracellular MAPK pathway.

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