Li, Wen-Zhen published the artcileDesign, synthesis, and biological evaluation of benzo[b]thiophene 1,1-dioxide derivatives as potent STAT3 inhibitors, Related Products of piperidines, the main research area is benzothiophene dioxide STAT3 inhibitor structure activity relationship; anticancer activity benzothiophene mol modeling; ROS; STAT3; apoptosis; cell cycle; inhibitors; mitochondrial membrane potential; tumors.
As a member of the signal transducer and activator of transcription (STAT) family, STAT3 plays a critical role in several biol. pathways such as cell proliferation, migration, survival, and differentiation. Due to abnormal continuous activation in tumors, inhibition of STAT3 has emerged as an attractive approach for the treatment of various cancer cells. Herein, we report a series of novel STAT3 inhibitors based on benzo[b]thiophene 1,1-dioxide scaffold and evaluated their anticancer potency. Among them, compound I exhibited the best activity against cancer cells. Compound I induced apoptosis and blocked the cell cycle. Meanwhile, I reduced intracellular ROS content and caused the loss of mitochondrial membrane potential. Further research revealed that I significantly blocked STAT3 phosphorylation and STAT3-dependent dual-luciferase reporter gene experiments showed that compound I has a marked inhibition of STAT3-mediated Firefly luciferase activity. Mol. modeling studies revealed compound I occupied the pocket well with the SH2 domain in a favorable conformation.
Chemical Biology & Drug Design published new progress about Antitumor agents. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Related Products of piperidines.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem