Synthesis and biologic activities of some novel heterocyclic chalcone derivatives

We synthesized 36 chalcone-like (E)-3-(substitutedphenyl)-1-hetrylprop-2-en-1-ones by condensing 2-acetylfuran/2-acetylpyrrole with substituted benzaldehydes under basic conditions. Of the 36 molecules synthesized, 10 are new to the literature. Bio-evaluation studies of these molecules revealed that compounds 5, 9, 15, 25, and 29 were potent NorA efflux pump inhibitors against Staphylococcus aureus by reducing MIC of ciprofloxacin fourfold, while compounds 11, 21, 25, and 26 showed promising anticancer activity in all four tested cancer cell lines (HL-60, MOLT-4, PC-3, and HeLa). Compound 25 emerged as a very good potentiator of ciprofloxacin against multidrug resistant S. aureus and also showed promising anticancer activity. The present communication describes syntheses, bio-evaluation, and structure-related activity of the (E)-3-(substitutedphenyl)-1-hetrylprop-2-en-1-ones.