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Paper | Regular issue | Vol 92, No. 2, 2016, pp.272-290
Published online, 15th January, 2016
DOI: 10.3987/COM-15-13329
Design, Synthesis, Antitumor and Antimicrobial Activity of Some Novel 6,7-Dimethoxyquinazoline Derivatives

Asmaa E. Kassab,* Ehab M. Gedawy, Zienab Mahmoud, and Rania A. Khattab

*Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 33 Kaser El Ainin Street 11562, Egypt


Novel 4-substituted-6,7-dimethoxyquinazolines 3, 4a and 4b were synthesized via reacting the corresponding 4-chloro derivative 2 with 2-(4-aminopiperazin-1-yl)ethanol, ethylpiperazine or benzylpiperidine. Quinazolines 6a-c and 8a-d were obtained through reacting 4-hydrazinylquinazoline 5 with different aromatic aldehydes or aromatic isothiocyanates. An attempt to synthesize 6,7-dimethoxyquinazolin-4-yl hydrazinecarboxamides via reacting the hydrazinyl derivative 5 with certain aromatic isocyanates was unsuccessful and the unexpected triazoloquinazoline 7 was obtained regardless to the isocyanate used .The anticancer activity of 4 compounds, namely 3, 4a, 4b and 7 was evaluated by National Cancer Institute (USA) at single dose (10-5 M) utilizing 59 different human tumor cell lines. Moreover, the antimicrobial activity of all the newly synthesized quinazolines was screened against Gram positive bacteria (Staphylococcus aureus and Bacillus subtilis), Gram negative bacteria (Escherichia coli and Klebsiella) and a fungal strain (Candida albicans).