| abstract |
The invention discloses a STAT3 small molecule inhibitor and its application, and provides a N'-(1-(2,4 dihydroxyphenyl)ethylene) represented by formula (1) or formula (1a) Benzohydrazide derivatives or pharmacologically acceptable salts thereof are STAT3 inhibitors as active ingredients. In the formula, R 1 and R 2 on ring A can be hydroxyl, methoxy, carboxyl and aliphatic, and B can be cyclic or chain. The small molecule inhibitor of STAT3 provided by the present invention has selectivity and high activity. According to the tertiary structure design of STAT3, it is biosynthesized and optimized, and then the activity is detected by methods such as fluorescence polarization and CCK-8, and the inhibitory effect of this type of inhibitor is studied. The mechanism of tumor cell growth, promotion of differentiation and apoptosis, so as to clarify the role of STAT3 small molecule inhibitors in preventing tumorigenesis and treating tumors. |