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Synthesis and antimalarial and antineoplastic activities of some derivatives of 2,4-diamino-5-methyl-6-substituted benzylaminoquinazolines

Meng, X.Y.; Zhang, X.P.; Li, B.S.; Li, G.D.

Yao Xue Xue Bao 24(8): 578-586

1989

ISSN/ISBN: 0513-4870
PMID: 2694758
Document Number: 328523
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.

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