Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 15, Issue 24, Pages 7677-7687Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.08.062
Keywords
PI3K; p110 alpha; sulfonohydrazide
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A series of 2-methyl-5-nitrobenzenesulfonohydrazides were prepared and evaluated as inhibitors of PI3K. An isoquinoline derivative shows good selectivity for the p110 alpha isoform over p110 beta and p110 delta, and also demonstrates good in vitro activity in a cell proliferation assay. Molecular modelling provides a rationalisation for the observed SAR. (c) 2007 Elsevier Ltd. All rights reserved.
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