Dihydrofuro[3,4-c]pyridinones as inhibitors of the cytolytic effects of the pore-forming glycoprotein perforin

Lena, G; Trapani, JA; Sutton, VR; Ciccone, A; Browne, KA; Smyth, MJ; Denny, William; Spicer, Julie

dc.contributor.author	Lena, G	en
dc.contributor.author	Trapani, JA	en
dc.contributor.author	Sutton, VR	en
dc.contributor.author	Ciccone, A	en
dc.contributor.author	Browne, KA	en
dc.contributor.author	Smyth, MJ	en
dc.contributor.author	Denny, William	en
dc.contributor.author	Spicer, Julie	en
dc.date.accessioned	2011-11-17T17:16:21Z	en
dc.date.issued	2008-12-11	en
dc.identifier.citation	Journal of Medicinal Chemistry 51(23):7614-7624 11 Dec 2008	en
dc.identifier.issn	0022-2623	en
dc.identifier.uri	http://hdl.handle.net/2292/9218	en
dc.description.abstract	Dihydrofuro[3,4-c]pyridinones are the first class of small molecules reported to inhibit the cytolytic effects of the lymphocyte toxin perforin. A lead structure was identified from a high throughput screen, and a series of analogues were designed and prepared to explore structure−activity relationships around the core bicyclic thioxofuropyridinone and pendant furan ring. This resulted in the identification of a submicromolar inhibitor of the perforin-induced lysis of Jurkat T-lymphoma cells.	en
dc.language	EN	en
dc.publisher	American Chemical Society	en
dc.relation.ispartofseries	Journal of 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/0022-2623/	en
dc.rights.uri	https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm	en
dc.subject	CYTOTOXIC T-LYMPHOCYTES	en
dc.subject	MEDIATED CYTOTOXICITY	en
dc.subject	CELL-DEATH	en
dc.subject	HEMOPHAGOCYTIC LYMPHOHISTIOCYTOSIS	en
dc.subject	DERIVATIVES	en
dc.subject	PATHWAY	en
dc.subject	MECHANISMS	en
dc.subject	ALLOGRAFTS	en
dc.subject	DISCOVERY	en
dc.subject	POTENT	en
dc.title	Dihydrofuro[3,4-c]pyridinones as inhibitors of the cytolytic effects of the pore-forming glycoprotein perforin	en
dc.type	Journal Article	en
dc.identifier.doi	10.1021/jm801063n	en
pubs.issue	23	en
pubs.begin-page	7614	en
pubs.volume	51	en
dc.rights.holder	Copyright: American Chemical Society	en
dc.identifier.pmid	19007200	en
pubs.end-page	7624	en
dc.rights.accessrights	http://purl.org/eprint/accessRights/RestrictedAccess	en
pubs.subtype	Article	en
pubs.elements-id	116352	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	Science	en
pubs.org-id	Science Research	en
pubs.org-id	Maurice Wilkins Centre (2010-2014)	en
pubs.record-created-at-source-date	2011-11-17	en
pubs.dimensions-id	19007200	en