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International Journal of Pharmaceutical Chemistry and Analysis


17-Oxo-17a-Aza-D-Homo-5-Androsten-3β-Yl Esters: Cytotoxic To Liver and Neuroblastoma Cancer Cell Lines


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Author Details: Neelima Dhingra1, T.R.Bhardwaj2

Volume : 2

Issue : 1

Online ISSN : 2394-2797

Print ISSN : 2394-2789

Article First Page : 14

Article End Page : 21


Abstract

 Introduction and positioning of the heteroatom in the parental steroid skeleton has significant effect on the activity profile of these compounds. A substantial amount of biologically relevant azasteroids have been reported as antifungals, antilipemic, neuromuscular blocking agents, local anaesthetics, antimicrobials, and GABA receptor antagonist. Recent work from our laboratory has described the synthesis and evaluation of 17-Oxo-17a-aza-D-homo-5-androsten-3β-yl ester derivatives as potential 5-alpha reductase inhibitors. The current study was undertaken to further investigate the cytotoxicity of the newly synthesized derivative using some more human cancer cell lines. Seven human cancer cell lines have been exposed to 1X 10-5m (single dose) of compounds (1-8), Finasteride, 5-fluorouracil, mitocycin 6 and, adriamycin were used as reference drugs for comparison. The cell growth was measured after 24h, using ELISA reader, after staining with sulforhodamine B dye (SRB), which binds to basic amino acid residues in the trichloroacetic acid (TCA) fixed cells. All the experiments were carried out in quadruplicate. The newly synthesized azasteroids derivatives displayed significant cytotoxicity against liver and neuroblastoma cell lines as compared to standard reference drugs. This together with, earlier reported antiproliferative activity against prostate cancer cell lines (DU-145) and 5-alpha reductase inhibitory activity, indicates that 17a-azasteroids seems to possess potential eliciting in vitro cytotoxicity. Results obtained from these studies shall be used as guidelines for further development of novel compounds to be used chemotherapeutic agents.

 

 

Keywords: Cytotoxicity; Human cancer cell lines; 17a-aza-D-Homosteroids; sulforhodamine B dye