Synthesis and evaluation of p-N,N-dialkyl substituted chalcones as anti-cancer agents

Grady Nelson, Mohammad A. Alam, Tyler Atkinson, Shirisha Gurrapu, J. Sravan Kumar, Chris Bicknese, Joseph L. Johnson, Michael Williams

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

Several new N,N-dialkyl substituted chalcones (chalconoids or benzylideneacetophenones) have been synthesized via the condensation of corresponding N,N-dialkylbenzaldehyde with various aryl methyl ketones. All the chalcones have been synthesized from readily available and cheap starting materials under environmentally benign conditions in very high yields without work up and column chromatographic purification. Synthesized compounds have been tested for their biological activity against pathogenic microorganisms such as Escherichia coli, Bacillus subtilis, and Mycobacterium smegmatis. Anti-cancer activity of these compounds has also been tested against multiple myeloma (RPMI-8226) and human mammary adenocarcinoma (MCF-7) cell lines. The most hydrophilic molecules 23 and 24 showed very good anti-cancer activity against MCF-7 cell lines at low micro-molar concentrations. All the compounds have also been evaluated for their activity against Beta-secretase 1 enzyme. One of the synthesized compounds showed Beta-secretase 1 enzyme inhibition activity at micro-molar concentration.

Original languageEnglish (US)
Pages (from-to)4610-4614
Number of pages5
JournalMedicinal Chemistry Research
Volume22
Issue number10
DOIs
StatePublished - Oct 1 2013

Keywords

  • Anti-cancer
  • Anti-microbial
  • Beta-secretase 1 enzyme
  • Chalcones

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