Title of article
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110α inhibitors Original Research Article
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
11
From page
7677
To page
7687
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.
Keywords
Sulfonohydrazide , PI3K , p110?
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2007
Journal title
Bioorganic and Medicinal Chemistry
Record number
1303852
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