title: Synthesis and biological evaluation of some quinazoline derivatives as antitumor and antiviral agents.
abstract: 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 (GI50) at concentrations of 3.2, 2.0, 4.8, 4.0 mumol/l 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-1 potency with EC50 values of 40.5 and 52.8 mumol/l, respectively. The detailed synthesis, spectroscopic and biological data are reported.
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. magda_m20@yahoo.com
authors.forename: Magda A
authors.initials: MA
authors.lastname: el-Sherbeny
authors.forename: Magdy M
authors.initials: MM
authors.lastname: Gineinah
authors.forename: Magda N
authors.initials: MN
authors.lastname: Nasr
authors.forename: Faiza S
authors.initials: FS
authors.lastname: el-Shafeih
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004354:Drug Screening Assays, Antitumor; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D014779:Virus Replication / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D000998:Antiviral Agents; D007202:Indicators and Reagents; D011799:Quinazolines