IBRAHIM M. ABDOU, SHAIKHA S. AL-NEYADI AND IHSAN SHEHADI, Department of Chemistry, Faculty of Science, UAE University, Al-Ain P.O. Box 17551 UAE; AHMED AL-MARZOUQI, Department of Biochemistry, Faculty of Medicine & Health Science, UAE University, Al-Ain P.O. Box 17666 UAE.
New series of substituted 2(1H)-pyridinones \textbf(1a-e) and their nucleosides \textbf(3a-e) were prepared as potential agents against leukemia. The nucleosides \textbf(2a-e) were synthesized using two independent methods and their structures were confirmed using FT-IR, 1D, and 2D-NMR techniques. 3-Cyano-4-(thien-2'-yl)-6-(4''-chlorophenyl)-2(1H)-pyridinone \textbf(1e) and its nucleoside (\textbf2e and \textbf3e) were found to have the highest activity against proliferation of the human promyelotic leukemia (HL-60) cells. Pyridinone derivatives substituted at position 4 with a 2-thienyl or 2-(trifluoromethyl)phenyl groups were found to exhibit high potency against apoptosis.