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

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.

A novel series of sulfonohydrazides were synthesised and evaluated for inhibition of isoforms of PI3K, and inhibition of cell proliferation. Molecular modelling helps to rationalise the observed SAR.Figure optionsDownload as PowerPoint slide