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


CONCLUSIONS
Compound 8 showed high anticancer and antiinflammatory activities, and is worth further studying.
Xu
L
L
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
Liu
J
J
Xu
S P
SP
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003110:Colonic Neoplasms / Q000473:pathology; D018922:HL-60 Cells / Q000187:drug effects; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008113:Liver Neoplasms / Q000473:pathology; D015394:Molecular Structure; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D007211:Indoles