Design, Synthesis and Biological Evaluation of Novel Benzo[4,5]thiazolo[2,3-c][1,2,4]triazole Derivatives as Potential Anticancer Agents

In the present study, we have designed and synthesized a novel series of benzothiazolotriazole derivatives as potential anticancer agents. The anticancer activity of the newly synthesized compounds was evaluated against three cancerous cell lines; A549 (human lung adenocarcinoma), MCF-7 (human breast carcinoma) and Hep3B (human hepatocellular carcinoma) using MTT assay. Among this series, compounds 15 and 16 showed the most promising anticancer activity with IC50 values between 11.1 to 21.5 μM. Kinase profiling was performed for the most potent compounds 15 and 16 and it revealed weak inhibitory activity against 10 various kinases, where the highest inhibition was against CDK2/Cyclin A1 by compound 15. Furthermore, caspase-3/7 assay also indicated that the same compound 15 has the ability to induce apoptosis through the activation of effector caspase-3/7 family. Therefore, it could be deduced that the S-benzo[4,5]thiazolo[2,3-c][1,2,4]triazole is a promising novel anticancer scaffold with antiproliferative and apoptosis-inducing activities deserves to be taken up as a lead for further structural optimization.