Roe, S., Gunaratnam, M., Spiteri, C. , Sharma, Pallavi, Alharthy, R. D., 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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| Item Type: | Article |
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| Item Status: | Live Archive |
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 |
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| 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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