Synthesis and antiandrogenic activity of some new 3-substituted androstano[17,16-c]-5′-aryl-pyrazoline and their derivatives

A series of androstano[17,16-c]pyrazolines and their oxidized derivatives (2-14) were synthesized using 3 beta-hydroxyandrostan-17-one as a starting material (1a, b). The synthesized compounds were evaluated for their antiandrogenic activity compared to that of Cyproterone (R) as positive control. Some of the compounds exhibited better antiandrogenic activity than the reference drug. The detailed synthesis, spectroscopic data, ED50, and toxicity (LD50 and LD90) of the synthesized compounds were reported. (c) 2005 Elsevier Ltd. All rights reserved.