Synthesis and anticancer activity of benzotriazole derivatives

Abstract

Abstract A series of benzotriazole (BTA) derivatives were synthesized as tyrosine protein kinase inhibitors using fragment‐based design strategy. All desired compounds were synthesized with the reaction of benzotriazole, chloroacetonitrile and aromatic aldehyde using Ultrasonic‐Microwave method and characterized by IR, 1 H and 13 C‐NMR, mass spectrometry (MS) and elemental analysis. The anticancer activity of these compounds was evaluated by CCK‐8 method against carcinoma VX2, lung cancer A549, stomach cancer cell lines MKN45 and MGC in vitro . The results showed that all compounds showed good antiproliferative activity. In particular, compound 2.1 showed the most prominent inhibition of VX2 cell lines with IC 50 of 3.80 ± 0.75 μM. Compound 2.2 exhibited highly potent anticancer activity of stomach MGC cell lines with IC 50 of 3.72 ± 0.11 μM. A549 and MKN45 cell lines were sensitive to compound 2.5 with IC 50 of 5.47 ± 1.11 and 3.04 ± 0.02 μM, respectively.