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

Abstract

A series of androstano[17,16-c]pyrazolines and their oxidized derivatives (2-14) were synthesized using 3beta-hydroxyandrostan-17-one as a starting material (1a, b). The synthesized compounds were evaluated for their antiandrogenic activity compared to that of Cyproterone as positive control. Some of the compounds exhibited better antiandrogenic activity than the reference drug. The detailed synthesis, spectroscopic data, ED(50), and toxicity (LD(50) and LD(90)) of the synthesized compounds were reported.