Abstract
A series of 2 '-mercapto-3 '-cyano-4 '-(aryl)-4-pregneno-[3,2-e] pyridine-20-ones (3a-h) and 1 '-thiocarbamoyl-2 '-amino-4 '-(aryl)-4-pregneno-[3,2-e] pyridine-20-one derivatives (4a-h) were synthesized using progesterone 1 "17-acetyl-1,7,8,10,11,12,13,15,16,17-decahydro-10,13-dimethyl-2Hcyclopenta[a]phenanthren-3(6H,9H,14H)-one" as starting material. The synthesized compounds were evaluated for 5 alpha-reductase inhibitors and anti-prostate cancer activities compared to Anastrozole (R) as positive control. Some of the tested compounds exhibited better activities than Anastrozole (R). Compounds 3a-h and 4a-h showed potent 5a-reductase inhibitors and anti-prostate cancer activities than Anastrozole (R)