Synthesis and Study of Antimitotic Activities of Novel Analogues of Podophyllotoxin

Abstract

Podophyllotoxin derivatives and analogues show conspicuous antimitotic and other biological activities. The present study was concentrated on synthesis of novel analogues of podophyllotoxinande their study of antimitotic activities. b-apopicropodophyllin analogues, 1- Hydroxy-2-hydroxylmethyl-3-carboxy-4-(p-tolyl)-6, 7-dimethoxy - 1,2,3,4-tetrahydronaphthalene, 6-methoxy-7-methyl-9-p-tolyl naphtho [2.3-C] furan-1- (3H, 4H, 9H) one, 7-Chloro-6-methoxy-9-p-tolyl naphtho [2, 3-C] furan-1- (3H, 4H, 9H) one and 9-Cyclohexyl-6, 7-dimethoxy naphtho- [2,3-C] furan-1- (3H, 4H, 9H) one were synthesized using tetralone esters and its derivatives. The structures were confirmed by Proton NMR, IR,Massspectroscopy and C H analysis. ID₅₀ 1.709x 10^-6M,1.862x 10^-6 M, 1.587x 10^-6 M and 1.784x 10^-6 M were relatively lower to that of Podophyllotoxin (I) and ß-apopicropodophyllin having ID₅₀ 4.290 x 10^-6M and 2.870 x 10^-6M shows more than 65%, a high inhibition activity to that parent compounds. Thus, new synthetic analogues find lot scopes in medicinal chemistry.