Synthesis and aromatase inhibitory activity of some new 16E-arylidenosteroids.

Bansal, Ranju; Thota, Sridhar; Karkra, Nalin; Minu, Maninder; Zimmer, Christina; Hartmann, Rolf W

dc.contributor.author	Bansal, Ranju
dc.contributor.author	Thota, Sridhar
dc.contributor.author	Karkra, Nalin
dc.contributor.author	Minu, Maninder
dc.contributor.author	Zimmer, Christina
dc.contributor.author	Hartmann, Rolf W
dc.date.accessioned	2013-01-23T15:18:03Z
dc.date.available	2013-01-23T15:18:03Z
dc.date.issued	2012-12
dc.identifier.citation	Synthesis and aromatase inhibitory activity of some new 16E-arylidenosteroids. 2012, 45:36-40 Bioorg. Chem.	en_GB
dc.identifier.issn	1090-2120
dc.identifier.pmid	23064126
dc.identifier.doi	10.1016/j.bioorg.2012.08.005
dc.identifier.uri	http://hdl.handle.net/10033/266712
dc.description.abstract	A new series of 16E-arylidene androstene derivatives has been synthesized and evaluated for aromatase inhibitory activity. The impact of various aryl substituents at 16 position of the steroid skeleton on aromatase inhibitory activity has been observed. The 16E-arylidenosteroids 6, 10 and 11 exhibited significant inhibition of the aromatase enzyme. 16-(4-Pyridylmethylene)-4-androstene-3,17-dione (6, IC(50): 5.2 μM) and 16-(benzo-[1,3]dioxol-5-ylmethylene)androsta-1,4-diene-3,17-dione (11, IC(50): 6.4 μM) were found to be approximately five times more potent in comparison to aminoglutethimide.
dc.language.iso	en	en
dc.rights	Archived with thanks to Bioorganic chemistry	en_GB
dc.title	Synthesis and aromatase inhibitory activity of some new 16E-arylidenosteroids.	en
dc.type	Article	en
dc.contributor.department	University Institute of Pharmaceutical Sciences, Sector-14, Panjab University, Chandigarh 160 014, India. ranju29in@yahoo.co.in	en_GB
dc.identifier.journal	Bioorganic chemistry	en_GB
refterms.dateFOA	2018-06-12T23:42:13Z
html.description.abstract	A new series of 16E-arylidene androstene derivatives has been synthesized and evaluated for aromatase inhibitory activity. The impact of various aryl substituents at 16 position of the steroid skeleton on aromatase inhibitory activity has been observed. The 16E-arylidenosteroids 6, 10 and 11 exhibited significant inhibition of the aromatase enzyme. 16-(4-Pyridylmethylene)-4-androstene-3,17-dione (6, IC(50): 5.2 μM) and 16-(benzo-[1,3]dioxol-5-ylmethylene)androsta-1,4-diene-3,17-dione (11, IC(50): 6.4 μM) were found to be approximately five times more potent in comparison to aminoglutethimide.