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The discovery of potent cRaf1 kinase inhibitors.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lackey K,Cory M,Davis R,Frye SV,Harris PA,Hunter RN,Jung DK,McDonald OB,McNutt RW,Peel MR,Rutkowske RD,Veal JM,Wood ER

doi

10.1016/s0960-894x(99)00668-x

subject

Has Abstract

pub_date

2000-02-07 00:00:00

pages

223-6

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(99)00668-X

journal_volume

10

pub_type

杂志文章

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