Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110α inhibitors

…, GW Rewcastle, R Frederick, C Mawson…

文献索引：Kendall, Jackie D.; Rewcastle, Gordon W.; Frederick, Raphael; Mawson, Claire; Denny, William A.; Marshall, Elaine S.; Baguley, Bruce C.; Chaussade, Claire; Jackson, Shaun P.; Shepherd, Peter R. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 24 p. 7677 - 7687

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被引用次数: 45

摘要

A series of 2-methyl-5-nitrobenzenesulfonohydrazides were prepared and evaluated as inhibitors of PI3K. An isoquinoline derivative shows good selectivity for the p110α isoform over p110β and p110δ, and also demonstrates good in vitro activity in a cell proliferation assay. Molecular modelling provides a rationalisation for the observed SAR.