Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: A legitimate approach

► A total of 19 novel steroidal 5α-reductase inhibitors were synthesized. ► In vitro biological evaluation against HEK cells was carried out. ► Compounds 21-23 and 25 were found to be potent 5α-reductase II inhibitors. ► Compound 13 was found to be potent inhibitor of 5α-reductase I enzyme.