compound 11b

Compound 11b is a novel piperidinyl-based benzoxazole derivative, specifically a p-fluorophenyl substituted analog, identified as a potent dual inhibitor of the receptor tyrosine kinases VEGFR-2 and c-Met. These kinases are critical mediators of tumor angiogenesis, growth, and metastasis. In preclinical studies, compound 11b demonstrated significant selective cytotoxicity against breast cancer (MCF-7), prostate cancer (PC-3), and lung cancer (A549) cell lines, with high selectivity for MCF-7 over normal breast cells. Mechanistically, the compound induces G2/M phase cell-cycle arrest and triggers apoptosis through the mitochondrial pathway, characterized by the upregulation of pro-apoptotic markers such as p53, BAX, and caspase-9, and the downregulation of the anti-apoptotic protein Bcl-2. Molecular docking studies suggest that compound 11b binds stably within the ATP-binding pockets of both VEGFR-2 and c-Met kinases.

Other names

p-fluorophenyl piperidinyl-based benzoxazole derivative