imidazolone and fosbretabulin

imidazolone has been researched along with fosbretabulin* in 1 studies

Other Studies

1 other study(ies) available for imidazolone and fosbretabulin

Article	Year
Imidazolone-amide bridges and their effects on tubulin polymerization in cis-locked vinylogous combretastatin-A4 analogues: synthesis and biological evaluation. Bioorganic & medicinal chemistry, 2011, Jun-01, Volume: 19, Issue:11 A series of novel combretastatin-A4 analogues in which the cis-olefinic bridge is replaced by an imidazolone-amide were synthesized, and their cytotoxicity and tubulin-polymerization inhibitory activities were evaluated. These compounds appear to be potential tubulin-polymerization inhibitors. Compounds 10, 9b and 9c, bearing 3'-NH₂-4'-OCH₃, 4'-CH₃ and 3'-CH₃-substituted 1-phenyl B-ring, confer optimal bioactivity. The binding modes of these compounds to tubulin were obtained by molecular docking, which can explain the compounds' structure-activity relationship. The studies presented here provide a new structural type for the development of novel antitumor agents. Topics: Amides; Binding Sites; Cell Line, Tumor; Computer Simulation; Humans; Imidazoles; Isomerism; Stilbenes; Structure-Activity Relationship; Tubulin; Tubulin Modulators	2011

Article

Year

Imidazolone-amide bridges and their effects on tubulin polymerization in cis-locked vinylogous combretastatin-A4 analogues: synthesis and biological evaluation.

Bioorganic & medicinal chemistry, 2011, Jun-01, Volume: 19, Issue:11

A series of novel combretastatin-A4 analogues in which the cis-olefinic bridge is replaced by an imidazolone-amide were synthesized, and their cytotoxicity and tubulin-polymerization inhibitory activities were evaluated. These compounds appear to be potential tubulin-polymerization inhibitors. Compounds 10, 9b and 9c, bearing 3'-NH₂-4'-OCH₃, 4'-CH₃ and 3'-CH₃-substituted 1-phenyl B-ring, confer optimal bioactivity. The binding modes of these compounds to tubulin were obtained by molecular docking, which can explain the compounds' structure-activity relationship. The studies presented here provide a new structural type for the development of novel antitumor agents.

Topics: Amides; Binding Sites; Cell Line, Tumor; Computer Simulation; Humans; Imidazoles; Isomerism; Stilbenes; Structure-Activity Relationship; Tubulin; Tubulin Modulators

2011