期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 10, 期 3, 页码 223-226出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(99)00668-X
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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. (C) 2000 Elsevier Science Ltd. All rights reserved.
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