Journal
ARCHIVES OF PHARMACAL RESEARCH
Volume 34, Issue 7, Pages 1055-1063Publisher
PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-011-0702-2
Keywords
Five alpha reductase enzyme; Benign prostatic hyperplasia; Androstane derivatives; Androgens; Prostate cell line
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Funding
- University Grants Commission, New Delhi
- Council of Scientific and Industrial Research, New Delhi
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A number of 17-oxo-5-androsten-3 beta-yl esters (9a-9f) and 3 beta-alkoxy-5-androsten-17-ones (11a-11e) were synthesized from commercially available (25R)-5-spirosten-3 beta-ol (Diosgenin) (4) as starting material. The synthesized compounds were evaluated for their antiproliferative activity against the prostate-specific cancer cell line DU-145, acute toxicity and effect on serum androgen levels, and compared with finasteride as positive control. Some of the compounds exhibited better cytotoxicity and antiandrogenic activity than the reference control. The detailed synthesis, spectroscopic data and biological activity of the synthesized compounds are reported.
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