2,4-二氨基-5-甲基-6-取代苄氨基喹唑啉衍生物的合成及其抗疟和抗肿瘤作用

本文报道2,4-二氨基-5-甲基-6-取代苄氨基喹唑啉衍生物的合成及其抗疟和抗肿瘤活性。这类化合物由5-甲基-2,4,6-三氨基喹唑啉与相应的取代苯甲醛缩合成Schiff碱,然后经还原,甲酰化或亚硝化制得。经对伯氏鼠疟原虫(Plasmodium berghei)抑制性治疗筛选,有三个化合物Ⅳ_(2,5,6)剂量5mg/kg×4d抑制率为100%;体外抗肿瘤活性以Ⅱ_7和Ⅳ_8最强,对L1210白血病细胞株的IC_(50)分别为3.910×10~(-3)μg/ml和6.172×10~(-3)μg/ml,与MTX相当。

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.