Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 17, Pages 5065-5068Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.034
Keywords
Checkpoint kinase 1; CHK1 inhibitor; Kinase; Selenophene; Indolin-2-one
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Funding
- Ministry of Economy Affairs of ROC (Taiwan)
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A series of selenophene derivatives 3 were synthesized as potential CHK1 inhibitors. The effects of substitution on the 4'- or 5'-position of selenophene moiety and shifting the hydroxyl group position on C6-phenolic ring of oxindole were explored. This study led to the discovery of the most potent CHK1 inhibitors 29-33 and 39-43, which had IC(50) values in the subnanomolar range. (C) 2010 Elsevier Ltd. All rights reserved.
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