Drug discovery of N-methyl-pyrazole derivatives as potent selective estrogen receptor degrader (SERD) for the treatment of breast cancer.

Nowadays, ERα is considered to be a primary target for the treatment of breast cancer, and selective estrogen receptor degraders (SERDs) are emerging as promising antitumor agents. By analysing ERα-SERDs complexes, the pharmacophore features of SERDs and the crucial protein-ligand interactions were identified. Then, by utilizing the scaffold-hopping and bioisosteres strategy, 23 novel derivatives were designed, synthesized and biologically evaluated.

Design, synthesis, and biological evaluation of oridonin derivatives as novel NLRP3 inflammasome inhibitors for the treatment of acute lung injury.

Acute lung injury (ALI) is a severe respiratory disorder closely associated with the excessive activation of the NLRP3 inflammasome. Oridonin (Ori), a natural diterpenoid compound, had been confirmed as a specific covalent NLRP3 inflammasome inhibitor, which was completely different from that of MCC950. However, the further clinical application of Ori was limited by its weak inhibitory activity against NLRP3 inflammasome (IC = 1240.

Design, synthesis, and biological evaluation of novel sesquiterpene lactone derivatives as PKM2 activators with potent anti-ulcerative colitis activities.

Pyruvate kinase isoform 2 (PKM2) is closely related to the regulation of Th17/Treg balance, which is considered to be an effective strategy for UC therapy. Parthenolide (PTL), a natural product, only possesses moderate PKM2-activating activity. Thus, five series of PTL derivatives are designed and synthesized to improve PKM2-activated activities and anti-UC abilities.

Structural Modulation on NiCo S Nanoarray by N Doping to Enhance 2e-ORR Selectivity for Photothermal AOPs and Zn-O Batteries*.

As a H O generator, a 2e oxygen reduction reaction active electrocatalyst plays an important role in the advanced oxidation process to degrade organic pollutants in sewage. To enhance the tendency of NiCo S towards the 2e reduction reaction, N atoms are doped in its structure and replace S . The result implies that this weakens the interaction between NiCo S and OOH*, suppresses O-O bond breaking and enhances H O selectivity.

Hydrophobic POM Electrocatalyst Achieves Low Voltage "Charge" in Zn-Air Battery Coupled with Bisphenol A Degradation.

Zn-air batteriesare a perspective power source for grid-storage. But, after they are discharged at1.1 to 1.