Abstract: Sixteen 2,4-diamino-G-(N-methyl-substituted benzylamino) quinazoline, (Ⅰ) were synthesized by two different methods. 2-Nitro-5-chloro-benzonitrile was treated with the appropriate N-methyl-substituted benzylamines and 1 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 (I_6,7.10,16) out of these compounds suppressed all the parasites when administered orally at the dose of 5mg/kg and produced more than 99% suppression at 2.5mg/kg. Eight compounds(I_{1,2,4,5,8～10,15}) were found to have antitumor effects against Leukemia cells in culture comparable with or superior to those of the positive control methotrexate.