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Bioorg Med Chem Lett. 2000 Feb 7;10(3):223-6.

The discovery of potent cRaf1 kinase inhibitors.

Author information

1
Glaxo Wellcome, Inc., Research Triangle Park, NC 27709, USA. kel8725@glaxowellcome.com

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.

PMID:
10698440
DOI:
10.1016/s0960-894x(99)00668-x
[Indexed for MEDLINE]

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