Abstract
A series of anthra[1,2-d]imidazole-6,11-dione derivatives were synthesized and evaluated for telomerase inhibition, hTERT expression and suppression of cancer cell growth in vitro. All of the compounds tested, except for compounds 4, 7, 16, 24, 27 and 28 were selected by the NCI screening system. Among them, compounds 16, 39, and 40 repressed hTERT expression without greatly affecting cell growth, suggesting for the selectivity toward hTERT expression. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase and polypharmacological targeting strategy.
Original language | English |
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Pages (from-to) | 29-41 |
Number of pages | 13 |
Journal | European Journal of Medicinal Chemistry |
Volume | 60 |
DOIs | |
Publication status | Published - Feb 2013 |
Externally published | Yes |
Keywords
- Imidazole-fused anthraquinones
- Polypharmacology
- SEAP assay
- TRAP assay
- Telomerase
ASJC Scopus subject areas
- Drug Discovery
- Pharmacology
- Organic Chemistry