Document Type
Article
Date of Original Version
2011
Department
Biomedical and Pharmaceutical Sciences
Abstract
Six classes of coumarin derivatives (i.e. 3-alkyl-4-methylcoumarins, pyranocoumarins, coumarin carboxamides, quaternary ammonium coumarins, 7-aminocoumarins, and 4-aminocoumarins) were synthesized and evaluated for inhibition of cell proliferation of colon adenocarcinoma (HT-29), breast carcinoma (MDA-MB-468 or MCF-7), and human ovarian adenocarcinoma (SK-OV-3) cells. C-3-Alkyl substituted analogs of 4-methylcoumarins and pyranocoumarins, 5 and 6, inhibited the cell proliferation of MDA-MB-468 and SK-OV-3 cells by 53-74%, while 3-decyl substituted pyranocoumarin 10 and triethyl substituted quaternary ammonium coumarin derivative 29 inhibited the cell proliferation of HT-29 and SK-OV-3 cells by 63-72% at a concentration of 50 μM. Among all the compounds studied, C-3 decyl substituted quaternary ammonium coumarin derivative 25 exhibited the highest Src kinase inhibition with an IC 50 value of 21.6 μM.
Citation/Publisher Attribution
Kathuria, A., Jalal, S., Tiwari, R.,Shirazi, A. N., Gupta, S., Kumar, S., Parang, K., & Sharma, S. K. (2011). Substituted Coumarin Derivatives: Synthesis and Evaluation of Antiproliferative and Src Kinase Inhibitory Activities. Chemistry Biology Interface. 1(2):279-296. Retrieved from http://cbijournal.com/images/paper-archive/october-2011-vol-1/Research-Paper-11.pdf
Available at: http://cbijournal.com/images/paper-archive/october-2011-vol-1/Research-Paper-11.pdf
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