期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 13, 期 31, 页码 8500-8504出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5ob01177a
关键词
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资金
- EPSRC
- AICR
- CRUK Programme Grant
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-mu M range.
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