SYNTHESIS AND ANTICANCER ACTIVITY OF 3-［(3′-METHYL-4′-(SUBSTITUTED PHENYL)-1′,3′-BUTADIENYL］ INDOLE DERIVATIVES / 药学学报

ABSTRACT

AIM　To study the synthesis and anticancer activity of 3-［(3′-methyl-4′-(substituted phenyl)-1′,3′-butadienyl］ indole derivatives. METHODS　Electrophilic-substitution, aldol-condensation, selective-reduction, phase-transfer Wittig reaction and hydrolysis reaction were used in the synthesis of the title compounds. RESULTS　Eleven compounds of 3-［(3′-methyl-4′-(substituted phenyl)-1′,3′-butadienyl］ indole were synthesized. They are new compounds. Compound 8 showed different inhibitory effects on HL-60, HCT-8 and Bel7402 cell lines in vitro, and its inhibitory rate of antiinflammation was 100％ at 10-5 mol*L-1 concentration. CONCLUSION　Compound 8 showed high anticancer and antiinflammatory activities, and is worth further studying.