Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors

Jackie Kendall, Gordon W Rewcastle, Raphael Frederick, Claire Mawson, William A Denny, Elaine S Marshall, Bruce C Baguley, Claire Chaussade, Shaun Jackson, Peter R Shepherd

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Abstract

A series of 2-methyl-5-nitrobenzenesulfonohydrazides were prepared and evaluated as inhibitors of PI3K. An isoquinoline derivative shows good selectivity for the p110alpha isoform over p110beta and p110delta, and also demonstrates good in vitro activity in a cell proliferation assay. Molecular modelling provides a rationalisation for the observed SAR.
Original languageEnglish
Pages (from-to)7677 - 7687
Number of pages11
JournalBioorganic & Medicinal Chemistry
Volume15
Issue number24
DOIs
Publication statusPublished - 2007

Cite this

Kendall, J., Rewcastle, G. W., Frederick, R., Mawson, C., Denny, W. A., Marshall, E. S., Baguley, B. C., Chaussade, C., Jackson, S., & Shepherd, P. R. (2007). Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors. Bioorganic & Medicinal Chemistry, 15(24), 7677 - 7687. https://doi.org/10.1016/j.bmc.2007.08.062