An effective and economical protocol was developed for the synthesis of 3-substituted indoles by one-pot three-component coupling reaction of a substituted salicylaldehyde, N-methylaniline and indole using [Hmim] HSO4 as a catalyst. All the synthesized derivatives were evaluated for inhibition of cancer cell. The initial assays indicated that some of the newly synthesized compounds displayed significantly good inhibition activities against human breast cancer cell (MCF7), cell lines compared with the control (Adriamysin), which might be developed as novel lead scaffold for potential anticancer agents.