Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams.

The 17-oxo-17a-aza-d-homo-5-androsten-3beta-yl esters (13-22) were synthesized from commercially available (25R)-5-spirosten-3beta-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. Copyright (c) 2010 Elsevier Masson SAS. All rights reserved.