Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110 alpha inhibitors

Kendall, Jackie; Rewcastle, Gordon; Frédérick, Raphaël; Mawson, Claire; Denny, William; Marshall, Elaine; Baguley, Bruce; Chaussade, Claire; Jackson, SP; Shepherd, Peter

dc.contributor.author	Kendall, Jackie	en
dc.contributor.author	Rewcastle, Gordon	en
dc.contributor.author	Frédérick, Raphaël	en
dc.contributor.author	Mawson, Claire	en
dc.contributor.author	Denny, William	en
dc.contributor.author	Marshall, Elaine	en
dc.contributor.author	Baguley, Bruce	en
dc.contributor.author	Chaussade, Claire	en
dc.contributor.author	Jackson, SP	en
dc.contributor.author	Shepherd, Peter	en
dc.date.accessioned	2011-11-18T02:16:59Z	en
dc.date.issued	2007	en
dc.identifier.citation	Bioorganic & Medicinal Chemistry 15(24):7677-7687 2007	en
dc.identifier.issn	0968-0896	en
dc.identifier.uri	http://hdl.handle.net/2292/9386	en
dc.description.abstract	A series of 2-methyl-5-nitrobenzenesulfono-hydrazides were prepared and evaluated as inhibitors of PI3K. An isoquinoline derivative shows good selectivity for the p110a isoform over p110b and p110d, and also demonstrates good in vitro activity in a cell proliferation assay. Molecular modelling provides a rationalisation for the observed SAR.	en
dc.language	EN	en
dc.publisher	Elsevier Ltd.	en
dc.relation.ispartofseries	Bioorganic & Medicinal Chemistry	en
dc.rights	Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. Details obtained from http://www.sherpa.ac.uk/romeo/issn/0968-0896/	en
dc.rights.uri	https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm	en
dc.subject	PI3K	en
dc.subject	p110 alpha	en
dc.subject	sulfonohydrazide	en
dc.subject	PHOSPHATIDYLINOSITOL 3-KINASE	en
dc.subject	P110-ALPHA INHIBITORS	en
dc.subject	CANCER	en
dc.subject	WORTMANNIN	en
dc.subject	MUTATIONS	en
dc.subject	MECHANISM	en
dc.subject	ALCOHOLS	en
dc.title	Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110 alpha inhibitors	en
dc.type	Journal Article	en
dc.identifier.doi	10.1016/j.bmc.2007.08.062	en
pubs.issue	24	en
pubs.begin-page	7677	en
pubs.volume	15	en
dc.rights.holder	Copyright: Elsevier Ltd.	en
dc.identifier.pmid	17869522	en
pubs.end-page	7687	en
dc.rights.accessrights	http://purl.org/eprint/accessRights/RestrictedAccess	en
pubs.subtype	Article	en
pubs.elements-id	72608	en
pubs.org-id	Medical and Health Sciences	en
pubs.org-id	Medical Sciences	en
pubs.org-id	Auckland Cancer Research	en
pubs.org-id	Molecular Medicine	en
pubs.org-id	Science	en
pubs.org-id	Science Research	en
pubs.org-id	Maurice Wilkins Centre (2010-2014)	en
pubs.record-created-at-source-date	2010-09-01	en
pubs.dimensions-id	17869522	en