Abstrakt

5α-reductase inhibitors and anti-prostate cancer activities of some synthesized 4`-(aryl)-4-pregneno[3,2-e]pyridinone derivatives

Abd El-Galil E Amr, Mohamed M Abdalla, Mohamed MM Hussein, Hany M Safwat, Mohamed H Elgamal

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 5α-reductase inhibitors and anti-prostate cancer activities compared to Anastrozole® as positive control. Some of the tested compounds exhibited better activities than Anastrozole®. Compounds 3a-h and 4a-h showed potent 5α-reductase inhibitors and anti-prostate cancer activities than Anastrozole®.