Discovery of novel Quinazoline based Thiazolotriazole hybrids as potential EGFR inhibitor: Synthesis, anticancer evaluation and in silico studies

Abstract

Significant efforts have been made to design and synthesize novel series of quinazoline based thiazolotriazole analogues (8a-8n) and examined for their anticancer activity against two cancer cell lines (MCF-7 & A549).  The in vitro anticancer activity assessment of these analogues against the EGFR tyrosine kinase revealed that six compounds 8d, 8e, 8f, 8j, 8m, and 8nexhibited efficacy against tested cell lines.The results showed that compounds 8d and 8e were more efficient than the standard erlotinib, although compounds 8m and 8n were equally effective. In silico investigations of compounds were also performed to detect their interactions with the EGFR receptor, and the energy estimates were consistent with the reported IC₅₀ values. Overall, this study highlighted the potential of the newly prepared analogues as promising leads for further development into anticancer drugs.