isoerianin has been researched along with fosbretabulin* in 3 studies
*fosbretabulin: a microtubule destabilizing agent isolated from Combretum caffrum; structure in first source [MeSH]
*fosbretabulin: a microtubule destabilizing agent isolated from Combretum caffrum; structure in first source [MeSH]
3 other study(ies) available for isoerianin and fosbretabulin
| Article | Year |
|---|---|
A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Fluorine; Humans; Models, Molecular; Molecular Structure; Polymerization; Stilbenes; Structure-Activity Relationship; Tubulin | 2018 |
Rapid synthesis of 4-arylchromenes from ortho-substituted alkynols: A versatile access to restricted isocombretastatin A-4 analogues as antitumor agents.
Potent anticancer 4-arylchromene agents 6, as restricted isoCA-4 analogues, were prepared with excellent yields by a rapid and versatile synthetic pathway. First, in the presence of PTSA in EtOH, a variety of arylalkynols 9 were transformed into substituted 4-chromanones 10 in a one pot procedure which include regioselective arylalkynols hydration, alcohol etherification, MOM-cleavage, and cyclization. Further palladium coupling reactions, using aryl halides and N-tosylhydrazones 11 gave access to a small library of functionalized 4-arylchromenes 6 with good yields. From this series of 4-arylchromenes, we have identified compound 6s which inhibit tubulin assembly at a micromolar level and demonstrate a remarkable nanomolar level of cytotoxicity against four human cancer cell lines. Docking studies showed that isoCA-4 and its restricted chromene analogue 6s adopt a similar positioning in the colchicine binding-site of tubulin. Topics: Alcohols; Antineoplastic Agents, Phytogenic; Benzopyrans; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; K562 Cells; Models, Molecular; Molecular Structure; Stilbenes; Structure-Activity Relationship; Tumor Cells, Cultured | 2015 |
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
Silicon-containing combretastatin analogs were designed, synthesized and evaluated for stability and biological activities. Among them, compound 31 exhibited strong tubulin polymerization-inhibitory activity and very potent tumor cell growth-inhibitory activity (IC50=0.007 μM) in MCF-7 cell proliferation assay. This compound also potently inhibited [(3)H]colchicine binding (90.7% inhibition at 3 μM). These activities were comparable to those of combretastatin A-4 (CA-4) (1). In addition, compound 31 was physico-chemically more stable than 1. These results suggest that a silicon linker can act as a bioisoster of a cis carbon-carbon double bond. Topics: Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Colchicine; Drug Design; Female; Humans; Silicon; Stilbenes; Tubulin; Tubulin Modulators | 2013 |