Synthesis and biological evaluation of some quinazoline derivatives as antitumor and antiviral agents

A new series of 4- (4-aryl-1-piperazinyl)quinazolines 4a-f, 4-(3-substituted phenylamino)quinazoline derivatives 5a-h, 2-methoxycarbonylphenylaminoquinazoline derivatives 6a, b, 2-hydrazinocarbonylphenylaminoquinazolines 7a, b and 2-aryl-1-(substituted 4-quinazolinyl)-1,4-dihydro-5-oxo-5H- 1,3,4-benzotriazepines 8a-j have been synthesized and tested for their antitumor and antiviral activities. Among them, compounds 5a-d exhibited broad spectrum antitumor activity with full panel median growth inhibition (GI(50)) at concentrations of 3.2, 2.0, 4.8, 4.0 mumol/I and total growth inhibition at concentrations of 56.5, 51.0, 63.0 and 73.0 mumol/l, respectively. Compounds 7a and 7b showed moderate selectivity toward leukemia cell line. On the other hand, compounds 8a and 8b showed moderate anti HIV- I potency with EC50 values of 40.5 and 52.8 mumol/l, respectively. The detailed synthesis, spectroscopic and biological data are reported.