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

doi:10.1016/j.bmc.2007.08.062

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

Australian Centre for Blood Diseases

Research output: Contribution to journal › Article › Research › peer-review

52 Citations (Scopus)

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 language	English
Pages (from-to)	7677 - 7687
Number of pages	11
Journal	Bioorganic & Medicinal Chemistry
Volume	15
Issue number	24
DOIs	https://doi.org/10.1016/j.bmc.2007.08.062
Publication status	Published - 2007

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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

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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.",

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

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doi = "10.1016/j.bmc.2007.08.062",

language = "English",

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T1 - Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors

AU - Kendall, Jackie

AU - Rewcastle, Gordon W

AU - Frederick, Raphael

AU - Mawson, Claire

AU - Denny, William A

AU - Marshall, Elaine S

AU - Baguley, Bruce C

AU - Chaussade, Claire

AU - Jackson, Shaun

AU - Shepherd, Peter R

PY - 2007

Y1 - 2007

N2 - 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.

AB - 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.

UR - http://www.sciencedirect.com/science/article/pii/S0968089607007717

U2 - 10.1016/j.bmc.2007.08.062

DO - 10.1016/j.bmc.2007.08.062

M3 - Article

VL - 15

SP - 7677

EP - 7687

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

SN - 0968-0896

IS - 24

ER -

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

Abstract

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