[Synthesis and anticancer activity of 3-[(3'-methyl-4'-(substituted phenyl)-1',3'-butadienyl] indole derivatives].

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.