Facile synthesis and anticancer activity of tetrazolyl‐benzothiazole derivatives

Abstract

AbstractWe herein reported a concise synthesis of a new class of tetrazolyl‐benzothiazoles (TBTs). This synthesis was achieved via a microwave‐assisted ANRORC method followed by an acid‐catalyzed [2 + 3] cycloaddition. The TBT core was elaborated with diverse substituents at the N‐1 or N‐2 position on the tetrazole ring to create a compound library for further bioactivity evaluation. The newly synthesized TBT‐based compounds were assessed for their inhibitory effects against human breast cancer cell lines, MCF‐7 and MDA‐MB‐231. Our results revealed that N‐2 substituted TBTs were generally more active than their N‐1 isomers, and 11g emerged as the most potent inhibitor with IC50 values of 5.3 and 10.4 μg/mL against MCF‐7 and MDA‐MB‐231, respectively. This study provides new insights into the synthesis and anticancer inhibitory activity of TBTs, highlighting their potential for future drug development.