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用两条不同路线合成了16个2,4-二氨基-6-(N-甲基-取代苄氨基)喹唑啉衍生物,其中13个未见报道。有4个化合物剂量5mg/kg对小鼠体内伯氏疟原虫(Plasmodium berghei)的抑制率达100%,2.5mg/kg的抑制率大于99%;有8个化合物对培养的L1210白血病细胞株的增殖抑制作用相当或优于阳性对照药物甲氨噗呤(MTX)。
Sixteen 2,4-diamino-6- (N-methyl-substituted benzylamino) quinazoline derivatives were synthesized using two different routes, of which 13 were not reported. Four compounds at a dose of 5 mg / kg had a 100% inhibition of Plasmodium berghei in mice and an inhibition rate of more than 99% at a dose of 2.5 mg / kg. Eight compounds were tested against cultured L1210 leukemia cell lines Inhibition of proliferation was comparable to or better than the positive control drug methotrexate (MTX).