Author/Authors :
Jackie D. Kendall، نويسنده , , Gordon W. Rewcastle، نويسنده , , Raphaël Frédérick، نويسنده , , Claire Mawson، نويسنده , , William A. Denny، نويسنده , , Elaine S. Marshall، نويسنده , , Bruce C. Baguley، نويسنده , , Claire Chaussade، نويسنده , , Shaun P. Jackson، نويسنده , , Peter R. Shepherd، نويسنده ,
Abstract :
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.
