Recent Advances in enhancer of zeste homolog 2 Inhibitors: Structural insights and therapeutic applications.

Enhancer of Zeste Homolog 2 (EZH2) is overexpressed in many malignancies and plays a critical role in cancer progression. Therefore, it is considered a promising target for therapeutic intervention. Although several EZH2 inhibitors have entered clinical trials, only one has received FDA approval.

The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif.

Rho-associated coiled-coil containing kinase (ROCK) plays an important role in inflammation. Herein, a series of compounds were designed and synthesized as ROCK inhibitors based on the structure-based drug design (SBDD) strategy and were evaluated for cytotoxicity, antioxidant activity and anti-inflammatory activity. Among them, compound DC24 was identified as the optimal hit in enzymatic screening with an IC value of 0.

Synthesis and biological evaluations of 8-biaryl-2,2-dimethylbenzopyranamide derivatives against Alzheimer's disease and ischemic stroke.

Alzheimer's disease, the commonest cause of dementia, is a growing global health concern with huge implications for individuals and society. Stroke has still been a significant challenge in clinics for a long time, which is the second leading cause of death in the world, especially ischemic stroke. Both Alzheimer's disease and stroke are closely related to oxidative stress and HIF-1 signaling pathways in nerve cells.