Abstract

ONE-POT SYNTHESIS OF 2-(CYCLOHEXYLAMINO)-6,7-DIHYDRO- 3-(2-HYDROXYPHENYL)-6,6-DIMETHYL-1H-INDOL-4(5H)-ONES AS POTENTIAL ANTICANCER AGENTS

Suresh C. Jadhavar, Hanmant M. Kasaraliker, Bhimrao C. Khade and Sudhakar R. Bhusare*

Abstract

An efficient method was described for the synthesis of 2- (cyclohexylamino)-6,7-dihydro-3-(2-hydroxyphenyl)-6,6-dimethyl- 1H-indol-4(5H)-ones catalyzed by [Hmim]HSO4. The one-pot synthesis was achieved via reaction of cyclohexyl isocyanide, substituted salicylaldehyde, dimedone and ammonium acetate in ethanol at room temperature condition. All synthesized derivatives were evaluated for inhibition of cancer cell. The obtained derivatives were evaluated for their in vitro antitumor activity against MCF-7 cell lines compared to the reference drug (Adrimycin). Compounds were found to be the most active against cell lines exhibiting IC50, TGI and GI50 values ranging MCF-7 cell lines.

Keywords: Anticancer activity ? Salicylaldehyde ? Cyclohexyl isocyanide ? Dimedone ? Indole-4(H)-ones.