SYNTHESIS AND ANTICANCER ACTIVITY OF 3-［(3′-METHYL-4′-(SUBSTITUTED PHENYL)-1′,3′-BUTADIENYL］ INDOLE DERIVATIVES
- VernacularTitle:3-(3′-甲基-4′-取代苯基-1′,3′-丁二烯基)吲哚类衍生物的合成及其抗癌活性
- Author:
Li XU
;
Jie LIU
;
Shiping XU
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2001;36(1):29-33
- CountryChina
- Language:Chinese
-
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.
