Journal
ARCHIV DER PHARMAZIE
Volume 344, Issue 2, Pages 111-118Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201000196
Keywords
Calcium channel antagonist activity; Cytotoxicity; 1,4-Dihydropyridines; 4-Hydroxycoumarins
Funding
- research council of Tehran University of Medical Sciences
- INSF (Iran National Sciences Foundation)
- Research Council of Shiraz University of Medical Sciences
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In the present work 15 new 1,4-dihydropyridines (DHPs) bearing a coumarin ring were synthesized and assessed on 4 different human cancer cell lines (HeLa, K562, LS180, and MCF-7). Although, all the derivatives were inactive on LS180 cell line, the results on other cells showed that these compounds had weak to moderate antitumoral activities and their IC50 ranged from 25 to > 100 mu M. Among the synthesized compounds, 7-(2-nitrophenyl)-8,9,10,12-tetrahydro-7H-chromeno[4,3-b]quinoline-6,8-dione (6a) demonstrated the highest activity (IC50 range in different cell lines: 25.4-58.6 mu M). Furthermore, the calcium channel antagonist activity of the derivatives, an undesired effect when these compounds are used as antitumoral agents, was much lower than nifedipine, a reference antagonist. In conclusion, this group of compounds seems to have promising biological properties and further investigation on this group could potentially lead to the discovery of cytotoxic agents with low calcium channel blocking activity.
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