Abstract
A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.
Original language | English |
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Pages (from-to) | 102-112 |
Number of pages | 11 |
Journal | European Journal of Medicinal Chemistry |
Volume | 50 |
DOIs | |
Publication status | Published - Apr 2012 |
Externally published | Yes |
Keywords
- Amidoanthraquinones
- NCI 60-cell panel assay
- SEAP assay
- TRAP assay
- Telomerase
- hTERT expression
ASJC Scopus subject areas
- Drug Discovery
- Pharmacology
- Organic Chemistry