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Synthesis and biological activities of 2,4-diamino-5-fluoro-6-substituted benzylamino quinazolines

Meng, X.Y.; Liu, J.Q.; Zhang, X.P.; Chen, X.H.; Yu, A.Z.; Dai, Z.R.

Yao Xue Xue Bao 29(4): 261-267

1994

ISSN/ISBN: 0513-4870
PMID: 7976341
Document Number: 424527
The title compounds were synthesized by condensation of 5- fluoro-2, 4, 6-triaminoquinazoline (6a) with various substituted benzaldehydes to produce the corresponding Schiff bases, followed by reduction. II and III were obtained by formylation and nitrosation of I, respectively, IV were obtained by reduction of II. Primary screening for suppressive therapeutic effects against P. berghei in mice showed that six of the twenty-two compounds produced 100% suppression when administered orally at dose of 1 mg cntdot kg-1. All compounds exhibited potent activity against L-1210 cell in vitro. Among them I-4 was more active than MTX. A number of compounds showed moderate activities against Diplococcus pneumoniae in in vitro tests.

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