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Ring A structural modified derivatives of withaferin A and the evaluation of their cytotoxic potential

IR@IIIM: CSIR-Indian Institute of Integrative Medicine, Jammu

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Title Ring A structural modified derivatives of withaferin A and the evaluation of their cytotoxic potential
 
Creator Yousuf, Syed Khalid
Majeed, Rabiya
Ahmad, Mudassier
Sangwan, Payare lal
Purnima, Basant
Saxsena, A.K.
Suri, K.A.
Mukherjee, Debaraj
Taneja, Subhash Chandra
 
Subject Chemical Sciences
 
Description 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.
 
Date 2011
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://iiim.csircentral.net/333/1/10.1016j.steroids.2011.05.012.pdf
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
 
Relation http://dx.doi.org/10.1016/j.steroids.2011.05.012
http://iiim.csircentral.net/333/