Design, Synthesis, and Evaluation of Pyrrolopyrazine-Substituted Benzoxazole/Benzothiazole Derivatives Targeting Aurora Kinase a in Mcf-7 Cells

Abstract

This study reports the synthesis, characterization, and biological evaluation of 19 benzoxazole/benzothiazole hybrids (19a-s). The compounds were synthesized through a multi-step process and structurally confirmed via NMR, elemental, and MS analyzes. Their antiproliferative effects were assessed on MCF-7 breast cancer and HME1 healthy epithelial cells. MTT assays identified 15 compounds with significant cytotoxic activity, among which 19e, 19g, 19i, 19j, and 19k exhibited high selectivity for MCF-7 cells. ELISA results demonstrated that 19g, 19i, 19j, and 19k significantly reduced AURKA protein levels in MCF-7 cells, while sparing healthy cells, suggesting their role in inhibiting cancer cell proliferation. These findings highlight 19g, 19i, 19j, and 19k as promising selective AURKA-targeted agents for breast cancer therapy.