[Synthesis and anticancer activity of 3-[(3'-methyl-4'-(substituted phenyl)-1',3'-butadienyl] indole derivatives]
1Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
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.
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