Yousuf, Syed Khalid and Majeed, Rabiya and Ahmad, Mudassier and Sangwan, Payare lal and Purnima, Basant and Saxsena, A.K. and Suri, K.A. and Mukherjee, Debaraj and Taneja, Subhash Chandra (2011) Ring A structural modified derivatives of withaferin A and the evaluation of their cytotoxic potential. Steroids, 76 (10-11). pp. 1213-1222. ISSN 0039128X

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Regio-/stereoselective Michael addition to ring A of withaferin-A was performed using an optimized reaction procedure to synthesise a library of 2,3-dihydro,3-�-substituted withaferin-A derivatives. The analogues thus obtained were evaluated for in vitro cytotoxicity against various human cancer cell lines.3-Azido analogue exhibited 35-fold increase (IC50 = 0.02–1.9 �M) in cytotoxicity against almost the entire cell lines tested when compared to the parent molecule. However, further modifications of 3-azido analogue with various alkynes under Husigen’s cycloaddition conditions generated a variety of triazole derivatives with reduced cytotoxicity.

Item Type: Article
Subjects: Chemical Sciences
Depositing User: Mr. Amit Nargotra
Date Deposited: 02 Jan 2012 12:09
Last Modified: 02 Jan 2012 12:09

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