Synthesis and evaluation of antimitotic activity of new tetralone acid analogues of podophyllotoxin

Abstract

The new tetralone acids I (R = H, F, Me, OMe, SMe) were synthesized as analogs of podophyllotoxin. They were prepd. by replacing 3,4,5-trimethoxyphenyl ring with cyclohexyl group in podophyllotoxin and 1,3-methylene dioxy ring with methoxy, hydrogen, Me, thiomethyl, and fluorine atoms. The analogs of podophyllotoxin were synthesized using Gensler's method with some changes in reagents and exptl. procedure. The synthesized I were screened for their antimitotic activity. It is noteworthy that compd. I (R = H) exhibited excellent antimitotic activity, I (R = Me, F) showed considerable activity and I (R = OMe, SMe) showed low activity.