2.50
Hdl Handle:
http://hdl.handle.net/10033/266712
Title:
Synthesis and aromatase inhibitory activity of some new 16E-arylidenosteroids.
Authors:
Bansal, Ranju; Thota, Sridhar; Karkra, Nalin; Minu, Maninder; Zimmer, Christina; Hartmann, Rolf W
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.
Affiliation:
University Institute of Pharmaceutical Sciences, Sector-14, Panjab University, Chandigarh 160 014, India. ranju29in@yahoo.co.in
Citation:
Synthesis and aromatase inhibitory activity of some new 16E-arylidenosteroids. 2012, 45:36-40 Bioorg. Chem.
Journal:
Bioorganic chemistry
Issue Date:
Dec-2012
URI:
http://hdl.handle.net/10033/266712
DOI:
10.1016/j.bioorg.2012.08.005
PubMed ID:
23064126
Type:
Article
Language:
en
ISSN:
1090-2120
Appears in Collections:
publications of the department drug design and optimization (HIPS]DDOP)

Full metadata record

DC FieldValue Language
dc.contributor.authorBansal, Ranjuen_GB
dc.contributor.authorThota, Sridharen_GB
dc.contributor.authorKarkra, Nalinen_GB
dc.contributor.authorMinu, Maninderen_GB
dc.contributor.authorZimmer, Christinaen_GB
dc.contributor.authorHartmann, Rolf Wen_GB
dc.date.accessioned2013-01-23T15:18:03Z-
dc.date.available2013-01-23T15:18:03Z-
dc.date.issued2012-12-
dc.identifier.citationSynthesis and aromatase inhibitory activity of some new 16E-arylidenosteroids. 2012, 45:36-40 Bioorg. Chem.en_GB
dc.identifier.issn1090-2120-
dc.identifier.pmid23064126-
dc.identifier.doi10.1016/j.bioorg.2012.08.005-
dc.identifier.urihttp://hdl.handle.net/10033/266712-
dc.description.abstractA 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.en_GB
dc.language.isoenen
dc.rightsArchived with thanks to Bioorganic chemistryen_GB
dc.titleSynthesis and aromatase inhibitory activity of some new 16E-arylidenosteroids.en
dc.typeArticleen
dc.contributor.departmentUniversity Institute of Pharmaceutical Sciences, Sector-14, Panjab University, Chandigarh 160 014, India. ranju29in@yahoo.co.inen_GB
dc.identifier.journalBioorganic chemistryen_GB

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