Publications by authors named "Shufu Wang"
Polyetheretherketone (PEEK) is widely used in orthopedic and dental implants due to its excellent mechanical properties, chemical stability, and biocompatibility. However, its inherently bioinert nature makes it present weak osteogenic activity, which greatly restricts its clinical adoption. Herein, strontium (Sr) is incorporated onto the surface of PEEK using mussel-inspired polydopamine coating to improve its osteogenic activity.
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- A series of novel 5-phenyl-1H-pyrazol derivatives were synthesized, including a cinnamamide moiety, to evaluate their potential as tubulin polymerization inhibitors.
- Compound 5j was identified as the most effective, showing an IC50 value of 1.02 μM, outperforming the reference drug Colchicine (IC50 = 1.34 μM).
- Docking simulations and a 3D-QSAR model were used to analyze the binding of compound 5j to tubulin and to aid in the design of more effective tubulin inhibitors.
Many reports implied that the BRAF serine/threonine kinase was mutated in various types of human tumors, which were related with cell growth, survival and differentiation. To provide new therapeutic opportunities, a series of novel 4,5-dihydro-1H-pyrazole derivatives (6a-10d) containing thiazole moiety as potential V600E mutant BRAF kinase (BRAF(V600E)) inhibitors were designed and synthesized. All compounds were evaluated in vitro for anticancer activities against WM266.
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- A series of 5-phenyl-1H-pyrazole derivatives, containing a niacinamide group, were synthesized and tested for their ability to inhibit the BRAF(V600E) enzyme.
- Compound 5h stood out as the most effective inhibitor, demonstrating a potent IC50 value of 0.33 μM, and showed good antiproliferative activity against melanoma cell lines WM266.4 and A375, closely matching the performance of the positive control vemurafenib.
- Molecular docking studies were conducted on compound 5h to analyze its binding interactions with BRAF(V600E), alongside 3D quantitative structure-activity relationship (QSAR) assessments to further
The kinesin spindle protein (KSP) is involved in the formation of bipolar mitotic spindle during cell division and it becomes a new target to overcome the neurotoxicity of MTs inhibitors. A series of flavone and isoflavone derivatives (1a-7c) have been designed, synthesized and evaluated as potential KSP inhibitors. Among them, 2c displayed the most potent inhibitory activity in vitro, which inhibited the growth of MCF-7 and Hela cell lines with IC50 values of 4.
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- The RAF-MEK-ERK signaling pathway is important for controlling the cell cycle and programmed cell death (apoptosis), with the BRAF(V600E) mutation causing constant activation that can disrupt normal cell growth.
- Researchers developed and tested new compounds, specifically 5-phenyl-1H-pyrazol derivatives, to inhibit the BRAF(V600E) mutant, finding that one compound (5c) was particularly effective with an IC50 value of 0.19 μM.
- In lab tests, compound 5c showed strong anti-cancer activity against melanoma cell lines, and its ability to bind to the BRAF(V600E) active site was confirmed through molecular docking