Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 6, Pages 2229-2236Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.01.064
Keywords
Dihydrotestosterone; Five alpha reductase enzyme; Benign prostatic hyperplasia; 17a-Aza steroids; Androgen
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Funding
- University Grants Commission, New Delhi
- Council of Scientific and Industrial Research, New Delhi
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The 17-oxo-17a-aza-D-homo-5-androsten-3 beta-yl esters (13-22) were synthesized from commercially available (25R)-5-spirosten-3 beta-ol (Diosgenin) (6) as starting material. The synthesized compounds were evaluated for their antiproliferative activity, acute toxicity and effect on serum androgen level and were compared with Finasteride as positive controls. Some of the compounds exhibited better cytotoxicity and antiandrogenic activity than the reference control. The detailed synthesis, spectroscopic data and pharmacological screening for the synthesized compounds were reported.
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