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  • Title: Synthesis and cytotoxic activity of 1-(3-oxoprop-1-enyl)-2-pyridones.
    Author: Ho LK, Knaus EE, Allen TM, Fathi-Afshar R.
    Journal: Drug Des Deliv; 1988 Feb; 2(3):227-37. PubMed ID: 3255317.
    Abstract:
    1-(3-Oxoprop-1-enyl) derivatives of nuclear substituted 2-pyridones (7a-i), 2-pyridinethione (7j), 1-isoquinolone (9), and the 1,4-dihydropyridine (11) have been synthesized and tested for biological activity. The 2-pyridones (7) and the 1-isoquinolone (9) were all active cytotoxic agents as determined in the in vitro L1210 screen, exhibiting activity in the ED50 0.5-3.5 micrograms/ml range. The nature and position of nuclear substituents present in 7 and 9 did not alter activity significantly. The unsubstituted (7a) and 5-ethoxycarbonyl-2-pyridones (7g), and the 1-isoquinolone derivative (9) were active antineoplastic agents (%T/C = 133-135) in vivo exhibiting activity comparable to 5-fluorouracil.
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