Antiproliferative Activity of Hybrid Compounds between 6-Methoxy-3-(4-methoxyphenyl)-1H-indole and 4-Phenylpiperidine against HCT-116 and HL-60 Cells

Indole derivatives have been potential anticancer drugs. Methyl 6-methoxy-3-(4-methoxypheny1)-1H-indole-2-carboxylate, in particular, was reported as a potent antiproliferative agent against MCF-7, NCI-H460, and A375-05 tumor cells. In this study, the 3-arylindole-2-carboxylate exhibited weak activity against HCT-116 colon tumor and HL-60 promyelocytic leukemia cells. To develop the potent antiproliferative indole derivatives against HCT-116 and HL-60 cells, we synthesized 6-methoxy-3-(4-methoxypheny1)-1H-indoles with various 2-substituents and assessed their activity. The 4-phenylpiperidine derivatives attenuated the tumor cells viability. Furthermore, their calculated structure resembled that of the antiproliferative loperamide derivatives.