Title

Substituted Coumarin Derivatives: Synthesis and Evaluation of Antiproliferative and Src Kinase Inhibitory Activities

Authors

Abha Kathuria
Sarah Jalal
Rakesh Tiwari, University of Rhode IslandFollow
Amir Nasrolahi Shirazi, University of Rhode Island
Shilpi Gupta
Shiv Kumar
Keykavous Parang, University of Rhode IslandFollow
Sunil K. Sharma

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