Development of Rofecoxib-Based Fluorescent Probes and Investigations on Their Solvatochromism, AIE Activity, Mechanochromism, and COX-2-Targeted Bioimaging

Cyclooxygenase-2 (COX-2) fluorescent probes are promising tools for early diagnosis of cancer. Traditionally, COX-2 were designed by connecting two parts, a fluorophore and binding unit, via flexible linker. Herein, new class COX-2-specific have been developed one-step modification from rofecoxib an integrative approach to combine the unit into one. Among them, several analogues not only exhibited still potent ability but also attractive fluorescence properties, such as tunable blue-red emission, solvatochromism, aggression-induced emission behavior, mechanochromism. Notably, 2a16 can be switched between green-yellow in crystalline state red-orange amorphous grinding fuming treatments. Furthermore, highly compound (?f = 0.94 powder) displayed much stronger imaging HeLa cancer cells overexpressing than RAW264.7 normal with minimal expression COX-2. Most importantly, light up human tissues adjacent brighter targeting enzyme. These results demonstrated potential red probe clinical applications.