Ah. Abadi et Ha. Alkhamees, 3-CYANO-4,6-DISUBSTITUTED-2(1H)-IMINO OR OXOPYRIDINES - NEW ANTINEOPLASTIC AGENTS WITH HIGH SELECTIVITY TOWARDS LEUKEMIA-CELL LINES, Archiv der pharmazie, 331(10), 1998, pp. 319-324
Two series of 3-cyano-2(1H)-oxopyridine and 3-cyano-2(1H)-iminopyridin
e derivatives carrying various aryl substituents at position 4 and (4-
((7-chloro or trifluoromethylquinol-4-yl)amino)phenyl) substituent at
position 6 were synthesized and evaluated for their antitumor activity
. Compounds 3f and 6d showed high selectivity towards leukemia cell li
nes with full panel median growth inhibition GI(50) average sensitivit
y towards all cell lines (MG-MID) at 7.9 and 19.7 mu M and leukemia su
bpanel GI(50) average sensitivity towards leukemia cell lines (MG-MLD)
at 1.74 and 2.9 mu M, respectively, also they exhibited full panel to
tal growth inhibition TGI (MG-MID) at 34.8 and 59.0 mu M and leukemia
subpanel TGI (MG-MID) at 5.3 and 13.5 mu M, respectively.