Several aromatic urea derivatives were designed and synthesized as DNA
-targeting agents, 4-amidylphenyl)amino-carbonyl]-2,6-diaminopyridine
(1) and 1,3-bis[5-(glycylamino)pyrid-2-yl]urea (3) showed remarkable D
NA-binding abilities as determined by ultrafiltration assay using calf
thymus DNA, their potencies being equal to and half that of netropsin
, respectively. Compound 1 inhibited the proliferation of both L1210 c
ells and KB cells with similar IC50 values to netropsin.