fosbretabulin has been researched along with naphthalene* in 3 studies
3 other study(ies) available for fosbretabulin and naphthalene
| Article | Year |
|---|---|
Conformationnally restricted naphthalene derivatives type isocombretastatin A-4 and isoerianin analogues: synthesis, cytotoxicity and antitubulin activity.
A novel series of dihydronaphtalene, tetrahydronaphtalene and naphtalene derivatives as restricted analogues of isoCA-4 were designed, synthesized and evaluated for their anticancer properties. High cell growth inhibition against four tumour cell lines was observed at a nanomolar level with dihydronaphtalenes 1d, e and 1h, tetrahydronaphtalene 2c and naphtalene 3c. Structure-activity relationships are also considered. These compounds exhibited a significant inhibitory activity toward tubulin polymerization (IC(50) = 2-3 μM), comparable to that of isoCA-4. The effect of the lead compounds 1e and 2c on the cancer cells tested was associated with cell cycle arrest in the G(2)/M phase. Docking studies reveal that these compounds showed a binding mode similar to those observed with their non-constraint isoCA-4 and isoerianin congeners. Topics: Antineoplastic Agents; Benzene; Bibenzyls; Cell Line, Tumor; Chlorophenols; Humans; Models, Molecular; Molecular Conformation; Naphthalenes; Peptides, Cyclic; Phenol; Protein Multimerization; Protein Structure, Quaternary; Tubulin; Tubulin Modulators | 2012 |
Synthesis and structure-activity relationships of 2-amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents.
A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC(50) values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine. Topics: Anisoles; Cell Line, Tumor; Cell Proliferation; Chemistry, Pharmaceutical; Drug Design; Drug Screening Assays, Antitumor; Humans; Indoles; Inhibitory Concentration 50; Models, Chemical; Naphthalenes; Neoplasms; Structure-Activity Relationship; Tubulin; Tubulin Modulators | 2008 |
Design, synthesis and cytotoxic activities of naphthyl analogues of combretastatin A-4.
The 3,4,5-trimethoxyphenyl and 3-hydroxy-4-methoxyphenyl rings of combretastatin A-4 are deemed optimal for its activity as antimitotic agent. The replacement of either one by a naphthalene ring results in compounds with a potency comparable to that of the parent compound. These results show that the naphthalene ring is a good surrogate for the 3,4,5-trimethoxyphenyl or the 3-hydroxy-4-methoxyphenyl rings of combretastatin A-4 and that neither of them is essential for the antitumor activity. Topics: Antineoplastic Agents; Naphthalenes; Stilbenes; Structure-Activity Relationship | 2000 |