ISSN: 0970-938X (Print) | 0976-1683 (Electronic)

Biomedical Research

An International Journal of Medical Sciences

Abstract

NAD(P)H: Quinone Oxidoreductase 1 inducer activity of some enaminone derivatives.

The present work reports the synthesis of some enaminone derivatives bearing the biologically active 3,4-dimethoxyphenyl (3) or 3,4,5-trimethoxyphenyl moieties (5 and 7), respectively. The trimethoxybenzene moiety has been previously reported to confer cytotoxic activity. However, we found that, at high micromolar concentrations, the new compounds have the ability to weak-ly induce the cytoprotective enzyme NQO1. This is most likely due to their electrophilic cyclo-hexenone functionality, a well-established structural feature of NQO1 inducers. The structure of the newly synthesized compounds was confirmed on the basis of elemental analyses, IR, 1H-NMR, 13C-NMR spectra.

Author(s): Mansour S. Alsaid, Mostafa M. Ghorab, Maureen Higgins, Albena T. Dinkova-Kostova, Abdelaaty A. Shahat
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