Synthesis and biological evaluation of hybrid acridine-HSP90 ligand conjugates as telomerase inhibitors

Roe, S. and Gunaratnam, M. and Spiteri, C. and Sharma, Pallavi and Alharthy, R. D. and Neidle, S. and Moses, J. E. (2015) Synthesis and biological evaluation of hybrid acridine-HSP90 ligand conjugates as telomerase inhibitors. Organic and Biomolecular Chemistry, 13 . pp. 8500-8504. ISSN 1477-0520

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Synthesis and biological evaluation of hybrid acridine-HSP90 ligand conjugates as telomerase inhibitors

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Abstract

The synthesis and biological evaluation of a series of bifunctional acridine-HSP90 inhibitor ligands as telomerase inhibitors is herein described. Four hybrid acridine-HSP90 inhibitor conjugates were prepared using a click-chemistry approach, and subsequently shown to display comparable results to the established telomerase inhibitor BRACO-19 in the TRAP-LIG telomerase assay. The conjugates also demonstrated significant cyctotoxity against a number of cancer cell lines, in the sub-μM range.

Keywords:Acridine-HSP90, Triazole, Click Chemistry, Telomerase, NotOAChecked
Subjects:F Physical Sciences > F160 Organic Chemistry
F Physical Sciences > F163 Bio-organic Chemistry
Divisions:College of Science > School of Chemistry
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ID Code:19606
Deposited On:20 Nov 2015 11:00

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