Novel aromatic urea derivatives with DNA-binding ability.
Several aromatic urea derivatives were designed and synthesized as DNA-targeting agents. N,N'-Dimethyl-N,N'-bis[(4-amidylphenyl)aminocarbonyl]-2,6-di aminopyridine (1) and 1,3-bis[5-(glycylamino)pyrid-2-yl]urea (3) showed remarkable DNA-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 cells and KB cells with similar IC50 values to netropsin.
Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
R
R
Fukutomi
H
H
Kagechika
Y
Y
Hashimoto
K
K
Shudo
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002417:Cattle; D002455:Cell Division / Q000187:drug effects; D004247:DNA / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D007624:KB Cells; D007700:Kinetics; D007939:Leukemia L1210; D009682:Magnetic Resonance Spectroscopy; D009429:Netropsin / Q000494:pharmacology; D014462:Ultrafiltration; D014508:Urea / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D009429:Netropsin; D014508:Urea; D004247:DNA