Zhou W C, Li G Y, Xin Z M, Li B S, Chen G D, Dai Z R, Zhang X P
Yao Xue Xue Bao. 1989;24(2):99-104.
Sixteen 2,4-diamino-6-(N-methyl-substituted benzylamino) quinazolines (I) were synthesized by two different methods. 2-Nitro-5-chloro-benzonitrile was treated with the appropriate N-methyl-substituted benzylamines and I was formed after reduction and cyclization. Another method was reductive methylation, i.e., 2,4-diamino-6-substituted benzylaminoquinazolines reacted with formaldehyde and sodium cyanoborohydride at pH 6.3. Suppressive therapeutic tests in mice infected with Plasmodium berghei showed that four (I6,7,10,16) out of these compounds suppressed all the parasites when administered orally at the dose of 5 mg/kg and produced more than 99% suppression at 2.5 mg/kg. Eight compounds (I1,2,4,5,8-10,15) were found to have antitumor effects against Leukemia cells in culture comparable with or superior to those of the positive control methotrexate.
通过两种不同方法合成了16种2,4 - 二氨基 - 6 -（N - 甲基取代苄基氨基）喹唑啉（I）。用适当的N - 甲基取代苄胺处理2 - 硝基 - 5 - 氯苯腈，经还原和环化后形成I。另一种方法是还原甲基化，即2,4 - 二氨基 - 6 - 取代苄基氨基喹唑啉在pH 6.3下与甲醛和氰基硼氢化钠反应。对感染伯氏疟原虫的小鼠进行的抑制性治疗试验表明，这些化合物中的四种（I6、7、10、16）以5mg/kg的剂量口服给药时可抑制所有寄生虫，在2.5mg/kg时产生超过99％的抑制作用。发现八种化合物（I1、2、4、5、8 - 10、15）在培养物中对白血病细胞具有抗肿瘤作用，与阳性对照甲氨蝶呤相当或优于甲氨蝶呤。
