Synthesis of 2-(2-(2-(Bis(2-chloroethyl)amino)ethoxy)benzylidene)benzofuran-3(2H)-one derivatives on the basis of benzaldehydes and acetophenones for its cytotoxic activity

Abstract

Benzofuranones and nitrogen mustards have reported alkylating properties, this work is aimed to synthesize some benzofuranones fused with nitrogen mustards. Substituted benzofuranones were synthesized by condensation of 2-hydroxy benzaldehydes and substituted 2-hydroxy acetophenones and further fused with nitrogen mustards gave high yields of target compounds 2-(2-(2-(Bis(2chloroethyl)amino)ethoxy)benzylidene)benzofuran-3(2H)-one derivatives. The synthesized compounds were characterized by FTIR, 1H NMR and LCMS spectral studies. Further, the synthesized compounds were subjected to 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay on A-549 and MCF-7 cell lines for its in-vitro cytotoxic activity. All the synthesized compounds showed promising cytotoxic activity in which AN-O-04 showed minimum CTC-50 proving its cytotoxic efficacy.

Keywords

• benzofuranone
• nitrogen mustard
• acetophenone
• mtt
• cytotoxicity