[Synthesis and antimalarial and antineoplastic activities of some derivatives of 2,4-diamino-5-methyl-6-substituted benzylaminoquinazolines].
This paper reports the synthesis and the antimalarial and anticancer activities of some derivatives of 2,4-diamino-5-methyl-6-substituted benzylaminoquinazolines. These compounds were synthesized by condensation of 5-methyl-2,4,6-triaminoquinazoline with substituted benzyaldehyde to produce Schiff base, followed by reduction, formylation or nitrosation. The suppressive therapeutic effects against Plasmodium berghei in mice showed that the suppressive rate of three compounds (IV 2,5,6)was 100 per cent at the dosage 5 mg/kg. The anticancer activity in vitro showed that II7 and IV3 had the strongest inhibition and their IC50 against L1210 Leukemia cell were 3.910 X 10(-3) micrograms/ml and 6.172 X 10(-3) micrograms/ml.
Meng
X Y
XY
Zhang
X P
XP
Li
B S
BS
Li
G D
GD
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials; D000970:Antineoplastic Agents; D007939:Leukemia L1210 / Q000473:pathology; D008288:Malaria / Q000188:drug therapy; D008545:Melanoma / Q000473:pathology; D051379:Mice; D010962:Plasmodium berghei; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000634:Aminoquinolines; D000962:Antimalarials; D000970:Antineoplastic Agents