883980-08-3Relevant academic research and scientific papers
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors
La Regina, Giuseppe,Bai, Ruoli,Rensen, Whilelmina Maria,Di Cesare, Erica,Coluccia, Antonio,Piscitelli, Francesco,Famiglini, Valeria,Reggio, Alessia,Nalli, Marianna,Pelliccia, Sveva,Da Pozzo, Eleonora,Costa, Barbara,Granata, Ilaria,Porta, Amalia,Maresca, Bruno,Soriani, Alessandra,Iannitto, Maria Luisa,Santoni, Angela,Li, Junjie,Miranda Cona, Marlein,Chen, Feng,Ni, Yicheng,Brancale, Andrea,Dondio, Giulio,Vultaggio, Stefania,Varasi, Mario,Mercurio, Ciro,Martini, Claudia,Hamel, Ernest,Lavia, Patrizia,Novellino, Ettore,Silvestri, Romano
, p. 123 - 149 (2013/03/13)
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.
ARYLTHIOINDOLE TUBULIN POLYMERIZATION INHIBITORS AND METHODS OF TREATING OR PREVENTING CANCER USING SAME
-
Page/Page column 39-40, (2010/11/08)
The present invention features arylthioindole compounds, pharmaceutical compositions of arylthioindole compounds and methods of treating a patient suffering from cancer or inflammatory, cardiac, or helminthic diseases, the method comprising administering
Arylthioindoles, potent inhibitors of tubulin polymerization
De Martino, Gabriella,La Regina, Giuseppe,Coluccia, Antonio,Edler, Michael C.,Barbera, Maria Chiara,Brancale, Andrea,Wilcox, Elizabeth,Hamel, Ernest,Artico, Marino,Silvestri, Romano
, p. 6120 - 6123 (2007/10/03)
Several arylthioindoles had excellent activity as inhibitors both of tubulin polymerization and of the growth of MCF-7 human breast carcinoma cells. Methyl 3-[(3,4,5-tri-methoxypheny)thio]-5-methoxy-1H-indole-2-carboxylate (21), the most potent derivative
