A Novel Arylurea Fatty Acid That Targets the Mitochondrion and Depletes Cardiolipin to Promote Killing of Breast Cancer Cells

Rawling, T; Choucair, H; Koolaji, N; Bourget, K; Allison, SE; Chen, YJ; Dunstan, CR; Murray, M

A Novel Arylurea Fatty Acid That Targets the Mitochondrion and Depletes Cardiolipin to Promote Killing of Breast Cancer Cells

Rawling, T

Choucair, H Koolaji, N Bourget, K Allison, SE Chen, YJ Dunstan, CR Murray, M

Permalink

Publication Type:: Journal Article
Citation:: Journal of Medicinal Chemistry, 2017, 60 (20), pp. 8661 - 8666
Issue Date:: 2017-10-26

Closed Access

	Filename	Description	Size
	C:\Users\040731\Documents\papers\published\2017, J Med Chem, Rawling\Med Chem Version\Revised\Final in template REVISED clean.pdf	Accepted Manuscript Version	402.68 kB	Adobe PDF	View/Open

Copyright Clearance Process

Recently Added
In Progress
Closed Access

This item is closed access and not available.

Full metadata record

Field	Value	Language
dc.contributor.author	Rawling, T https://orcid.org/0000-0002-6624-6586	en_US
dc.contributor.author	Choucair, H	en_US
dc.contributor.author	Koolaji, N	en_US
dc.contributor.author	Bourget, K	en_US
dc.contributor.author	Allison, SE	en_US
dc.contributor.author	Chen, YJ	en_US
dc.contributor.author	Dunstan, CR	en_US
dc.contributor.author	Murray, M	en_US
dc.date.issued	2017-10-26	en_US
dc.identifier.citation	Journal of Medicinal Chemistry, 2017, 60 (20), pp. 8661 - 8666	en_US
dc.identifier.issn	0022-2623	en_US
dc.identifier.uri	http://hdl.handle.net/10453/119734
dc.description.abstract	© 2017 American Chemical Society. Cancer cell mitochondria are promising anticancer drug targets because they control cell death and are structurally and functionally different from normal cell mitochondria. We synthesized arylurea fatty acids and found that the analogue 16-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)hexadecanoic acid (13b) decreased proliferation and activated apoptosis in MDA-MB-231 breast cancer cells in vitro and in vivo. In mechanistic studies 13b emerged as the prototype of a novel class of mitochondrion-targeted agents that deplete cardiolipin and promote cancer cell death.	en_US
dc.relation	http://purl.org/au-research/grants/nhmrc/GNT1087248
dc.relation.ispartof	Journal of Medicinal Chemistry	en_US
dc.relation.isbasedon	10.1021/acs.jmedchem.7b00701	en_US
dc.subject.classification	Medicinal & Biomolecular Chemistry	en_US
dc.subject.mesh	Cell Line, Tumor	en_US
dc.subject.mesh	Mitochondria	en_US
dc.subject.mesh	Animals	en_US
dc.subject.mesh	Humans	en_US
dc.subject.mesh	Mice	en_US
dc.subject.mesh	Breast Neoplasms	en_US
dc.subject.mesh	Urea	en_US
dc.subject.mesh	Fatty Acids	en_US
dc.subject.mesh	Xenograft Model Antitumor Assays	en_US
dc.subject.mesh	Apoptosis	en_US
dc.subject.mesh	Female	en_US
dc.subject.mesh	Mitochondrial Membranes	en_US
dc.title	A Novel Arylurea Fatty Acid That Targets the Mitochondrion and Depletes Cardiolipin to Promote Killing of Breast Cancer Cells	en_US
dc.type	Journal Article
utslib.citation.volume	20	en_US
utslib.citation.volume	60	en_US
utslib.for	0304 Medicinal and Biomolecular Chemistry	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
utslib.for	0305 Organic Chemistry	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Faculty of Science
pubs.organisational-group	/University of Technology Sydney/Faculty of Science/School of Mathematical and Physical Sciences
utslib.copyright.status	closed_access
pubs.issue	20	en_US
pubs.publication-status	Published	en_US
pubs.volume	60	en_US

Abstract:

© 2017 American Chemical Society. Cancer cell mitochondria are promising anticancer drug targets because they control cell death and are structurally and functionally different from normal cell mitochondria. We synthesized arylurea fatty acids and found that the analogue 16-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)hexadecanoic acid (13b) decreased proliferation and activated apoptosis in MDA-MB-231 breast cancer cells in vitro and in vivo. In mechanistic studies 13b emerged as the prototype of a novel class of mitochondrion-targeted agents that deplete cardiolipin and promote cancer cell death.

Please use this identifier to cite or link to this item:

http://hdl.handle.net/10453/119734