vinorelbine and Rhabdomyosarcoma

vinorelbine has been researched along with Rhabdomyosarcoma* in 1 studies

Other Studies

1 other study(ies) available for vinorelbine and Rhabdomyosarcoma

Article	Year
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors. Journal of medicinal chemistry, 2013, Jan-10, Volume: 56, Issue:1 New arylthioindole derivatives having different cyclic substituents at position 2 of the indole were synthesized as anticancer agents. Several compounds inhibited tubulin polymerization at submicromolar concentration and inhibited cell growth at low nanomolar concentrations. Compounds 18 and 57 were superior to the previously synthesized 5. Compound 18 was exceptionally potent as an inhibitor of cell growth: it showed IC₅₀ = 1.0 nM in MCF-7 cells, and it was uniformly active in the whole panel of cancer cells and superior to colchicine and combretastatin A-4. Compounds 18, 20, 55, and 57 were notably more potent than vinorelbine, vinblastine, and paclitaxel in the NCI/ADR-RES and Messa/Dx5 cell lines, which overexpress P-glycoprotein. Compounds 18 and 57 showed initial vascular disrupting effects in a tumor model of liver rhabdomyosarcomas at 15 mg/kg intravenous dosage. Derivative 18 showed water solubility and higher metabolic stability than 5 in human liver microsomes. Topics: Animals; Antineoplastic Agents; Caco-2 Cells; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Cytochrome P-450 Enzyme Inhibitors; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Humans; Imidazoles; Indoles; Liver Neoplasms; Membrane Potential, Mitochondrial; Mice; Microsomes, Liver; Mitosis; Permeability; Polymerization; Pyridines; Reactive Oxygen Species; Rhabdomyosarcoma; Solubility; Structure-Activity Relationship; Tubulin; Tubulin Modulators	2013

Article

Year

Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.

Journal of medicinal chemistry, 2013, Jan-10, Volume: 56, Issue:1

New arylthioindole derivatives having different cyclic substituents at position 2 of the indole were synthesized as anticancer agents. Several compounds inhibited tubulin polymerization at submicromolar concentration and inhibited cell growth at low nanomolar concentrations. Compounds 18 and 57 were superior to the previously synthesized 5. Compound 18 was exceptionally potent as an inhibitor of cell growth: it showed IC₅₀ = 1.0 nM in MCF-7 cells, and it was uniformly active in the whole panel of cancer cells and superior to colchicine and combretastatin A-4. Compounds 18, 20, 55, and 57 were notably more potent than vinorelbine, vinblastine, and paclitaxel in the NCI/ADR-RES and Messa/Dx5 cell lines, which overexpress P-glycoprotein. Compounds 18 and 57 showed initial vascular disrupting effects in a tumor model of liver rhabdomyosarcomas at 15 mg/kg intravenous dosage. Derivative 18 showed water solubility and higher metabolic stability than 5 in human liver microsomes.

Topics: Animals; Antineoplastic Agents; Caco-2 Cells; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Cytochrome P-450 Enzyme Inhibitors; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Humans; Imidazoles; Indoles; Liver Neoplasms; Membrane Potential, Mitochondrial; Mice; Microsomes, Liver; Mitosis; Permeability; Polymerization; Pyridines; Reactive Oxygen Species; Rhabdomyosarcoma; Solubility; Structure-Activity Relationship; Tubulin; Tubulin Modulators

2013