fosbretabulin has been researched along with pyrazole* in 3 studies
3 other study(ies) available for fosbretabulin and pyrazole
| Article | Year |
|---|---|
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
Topics: Animals; Antineoplastic Agents; Apoptosis; Benzimidazoles; Cell Cycle Checkpoints; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; HEK293 Cells; Hepatocytes; Humans; Mice; Molecular Docking Simulation; Molecular Structure; Polymerization; Pyrazoles; Structure-Activity Relationship; Sulfonamides; Tubulin; Tubulin Modulators | 2019 |
Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
The combretastatins are an important class of tubulin-binding agents. Of this family, a number of compounds are potent tumor vascular disrupting agents (VDAs) and have shown promise in the clinic for cancer therapy. We have developed a modular synthetic route to combretastatin analogs based on a pyrazole core through highly regioselective alkyne cycloaddition reactions of sydnones. These compounds show modest to high potency against human umbilical vein endothelial cell proliferation. Moreover, evidence is presented that these novel VDAs have the same mode of action as CA4P and bind reversibly to β-tubulin, believed to be a key feature in avoiding toxicity. The most active compound from in vitro studies was taken forward to an in vivo model and instigated an increase in tumor cell necrosis. Topics: Angiogenesis Inhibitors; Animals; Antineoplastic Agents, Phytogenic; Apoptosis; Cell Proliferation; Cells, Cultured; Dose-Response Relationship, Drug; Female; Human Umbilical Vein Endothelial Cells; Humans; Mice; Mice, SCID; Molecular Structure; Neoplasms, Experimental; Pyrazoles; Stilbenes; Structure-Activity Relationship; Sydnones | 2016 |
Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents.
A series of novel 5-phenyl-1H-pyrazol derivatives (5a-5x) containing cinnamamide moiety were synthesized and their biological activities as potential tubulin polymerization inhibitors were evaluated. Among them, compound 5j exhibited the most potent inhibitory activity with an IC50 value of 1.02 μM for tubulin, which was superior to that of Colchicine (IC50 = 1.34 μM). Docking simulation was performed to insert compound 5j into the crystal structure of tubulin at colchicine binding site to determine the probable binding model. 3D-QSAR model was also built to provide more pharmacophore understanding that could be used to design new agents with more potent tubulin inhibitory activity. Topics: Catalytic Domain; Cell Line, Tumor; Chemistry Techniques, Synthetic; Cinnamates; Humans; Inhibitory Concentration 50; Molecular Docking Simulation; Pyrazoles; Quantitative Structure-Activity Relationship; Tubulin; Tubulin Modulators | 2015 |