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Issue 31, 2015
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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.

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

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Publication details

The article was received on 10 Jun 2015, accepted on 30 Jun 2015 and first published on 09 Jul 2015


Article type: Paper
DOI: 10.1039/C5OB01177A
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Org. Biomol. Chem., 2015,13, 8500-8504

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

    S. Roe, M. Gunaratnam, C. Spiteri, P. Sharma, R. D. Alharthy, S. Neidle and J. E. Moses, Org. Biomol. Chem., 2015, 13, 8500
    DOI: 10.1039/C5OB01177A

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