Archives of Pharmacal Research 2011-07-01

Synthesis, antiproliferative activity, acute toxicity and assessment of the antiandrogenic activities of new androstane derivatives.

Neelima Dhingra, T R Bhardwaj, Neeraj Mehta, Tapas Mukhopadhyay, Ashok Kumar, Manoj Kumar

文献索引：Arch. Pharm. Res. 34(7) , 1055-63, (2011)

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摘要

A number of 17-oxo-5-androsten-3β-yl esters (9a-9f) and 3β-alkoxy-5-androsten-17-ones (11a-11e) were synthesized from commercially available (25R)-5-spirosten-3β-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.