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 3β-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, ED50, and toxicity (LD50 and LD90) of the synthesized compounds were reported.

A series of androstano[17,16-c]pyrazolines and their oxidized derivatives were synthesized by using 3β-hydroxyandrostan-17-one as starting material.Figure optionsDownload as PowerPoint slide