Synthesis and antileukemic activity of 16E-[4-(2-carboxy)ethoxybenzylidene]-androstene amides.

Ranju Bansal, Pratap Chandra Acharya

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160 014, India. ranju29in@yahoo.co.in

Steroids 2012 Apr

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In order to determine the structural requirements for cytotoxicity against various tumor cell lines, a new series of 16E-arylidene androstene amides with varying degrees of unsaturation in ring A has been synthesized. Characterization and invitro cytotoxic studies of the newly synthesized compounds are discussed. The compounds on evaluation against various tumor cell lines exhibited significant growth inhibition on leukemia cell lines. 3-Chloro-16E-{[4-(4-methylpiperazin-1-yl)-2-oxoethoxy]benzylidene}androst-5-en-17-one (10) emerged as the most potent compound of the series with GI(50) values of 3.94, 2.61, 6.90 and 1.79μM against CCRF-CEM, K-562, RPMI-8226 and SR leukemia cell lines, respectively. Copyright Â© 2012 Elsevier Inc. All rights reserved.

Citation

Ranju Bansal, Pratap Chandra Acharya. Synthesis and antileukemic activity of 16E-[4-(2-carboxy)ethoxybenzylidene]-androstene amides. Steroids. 2012 Apr;77(5):552-7