Roe, S., Gunaratnam, M., Spiteri, C., Sharma, P., Alharthy, R. D., Neidle, S., Moses, J. E. (August 2015) Synthesis and biological evaluation of hybrid acridine-HSP90 ligand conjugates as telomerase inhibitors. Org Biomol Chem, 13 (31). pp. 8500-4. ISSN 1477-0520
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.
| Item Type: | Paper |
|---|---|
| Additional Information: | Organic & biomolecular chemistry |
| CSHL Authors: | |
| Communities: | CSHL labs > Moses lab |
| Depositing User: | Matthew Dunn |
| Date: | 21 August 2015 |
| Date Deposited: | 08 Jan 2021 18:21 |
| Last Modified: | 08 Jan 2021 18:21 |
| URI: | https://repository.cshl.edu/id/eprint/39563 |
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