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New series of substituted 2(1$H$)-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(1$H$)-pyridinone \textbf{(1e)} and its nucleoside (\textbf{2e} and \textbf{3e}) 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.