Structure-based design, synthesis and evaluation of novel anthra[1,2-d]imidazole-6,11-dione derivatives as telomerase inhibitors and potential for cancer polypharmacology
Journal
European Journal of Medicinal Chemistry
Journal Volume
60
Pages
29-41
Date Issued
2013
Author(s)
Chen C.-L.
Chang D.-M.
Chen T.-C.
Lee C.-C.
Hsieh H.-H.
Huang F.-C.
Huang K.-F.
Huang H.-S.
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.
SDGs
Type
journal article