Synthesis and biological evaluation of novel 2-(2-arylmethylene)hydrazinyl- 4-aminoquinazoline derivatives as potent antitumor agents

Article abstract of DOI:10.1016/j.ejmech.2012.05.039

Two series of novel 2-(2-arylmethylene)hydrazinyl-4-aminoquinazoline derivatives were synthesized and evaluated for their cytotoxicity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. Most compounds displayed moderate to excellent activity, with IC₅₀ values ranging from 0.015 to 4.09 μM against all tested cell lines, respectively. The most promising compound 9p (E)-2-(2-((1-(2,3-dichlorobenzyl)-1H-imidazol-2-yl)methylene) hydrazinyl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine with IC₅₀ values of 0.031 μM, 0.015 μM, 0.53 μM and 0.58 μM, which was 4- to 224 times more active than references 10 and Iressa, had emerged as a lead for further structural modifications.