In Vitro Cytotoxicity Evaluation of a New Series of Benzo[g][1,2,4]triazolo[1,5-alpha]quinazolines

A series of twenty four benzo[g]triazoloquinazolines was prepared and fully characterized in our previous paper. Here, the cytotoxicity of these compounds was evaluated in vitro against three tumor cell lines, i.e. hepatocellular carcinoma (Hep-G2), human cervical cancer (Hela) and medulloblastoma (Daoy). MTT assay was employed to elucidate the cytotoxicity of the target molecules and dasatinib used as reference drug. It has been shown that compound 21 exhibited remarkable significant cytotoxicity against all tested cell lines with IC50 values ranged between 20.91 and 27.81 mu g/mL in relation to dasatinib (6.91-16.22 mu g/mL). Whereas compound 16 showed the highest activity against Hela and Hep-G2 with IC50 values of 4.57 and 7.37 mu g/mL, respectively, however compound 22 revealed significant cytotoxicity, showing IC50 values of 26.78 and 10.90 mu g/mL. Moreover, compound 15 was found to possess good activity against Daoy cell with IC50 value of 23.02 mu g/mL in regards to that of dasatinib (9.20 mu g/mL). In terms of selectivity, compound 15 was active against Daoy cell, while 17 and 20 against Hep-G2. Furthering study on structure modification of these compounds could be useful as templates to design more potent antitumor agents.