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ChemMedChem. 2009 Oct;4(10):1657-67. doi: 10.1002/cmdc.200900238.

Rapid evaluation of Antrodia camphorata natural products and derivatives in tumourigenic liver progenitor cells with a novel cell proliferation assay.

Author information

1
The School of Biomedical, Biomolecular & Chemical Sciences, The University of Western Australia, Crawley, Crawley, WA 6009 (Australia). sgs@cyllene.uwa.edu.au

Abstract

We report the syntheses of five natural product maleimide and maleic anhydrides from the mushroom Antrodia camphorata. The ability of these compounds to affect proliferation in non-tumourigenic and tumourigenic liver progenitor cell lines was monitored by the Cellscreen system, a novel and nondestructive rapid-screening instrument. Additionally, a range of new aryl-functionalised differentiated derivatives were prepared through a Suzuki cross-coupling reaction to influence cell-growth effects. Several derivatives radically slowed the proliferation of liver progenitor cells; however, of particular interest were two maleic anhydride derivatives containing aryl tethers. These analogues demonstrated selectivity for limiting the proliferation of tumourigenic progenitor cells in comparison with their non-tumourigenic counterparts. Also highlighted is the application of the Cellscreen system in medicinal chemistry to rapidly measure the effect of compound libraries on cell proliferation.

PMID:
19731279
DOI:
10.1002/cmdc.200900238
[Indexed for MEDLINE]

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