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

Authors

Abha Kathuria, University of Delhi
Sarah Jalal, University of Delhi
Rakesh Tiwari, Chapman UniversityFollow
Amir Nasrolahi Shirazi, Chapman UniversityFollow
Shilpi Gupta, University of Delhi
Shiv Kumar, University of Delhi
Keykavous Parang, Chapman UniversityFollow
Sunil K. Sharma, University of Delhi

Document Type

Article

Publication Date

2011

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.

Comments

This article was originally published in Chemistry & Biology Interface, volume 1, issue 2, in 2011.

Recommended Citation

Kathuria, Abha, Sarah Jalal, Rakesh Tiwari, Amir Nasrolahi Shirazi, Shilpi Gupta, Shiv Kumar, Keykavous Parang, and Sunil K. Sharma. "Substituted Coumarin Derivatives: Synthesis and Evaluation of Antiproliferative and Src Kinase Inhibitory Activities." Chemistry & Biology Interface 1.2 (2011): 279-296.

Copyright

Indian Society of Chemists and Biologists