116757-24-5Relevant academic research and scientific papers
Iodine-promoted selective 3-selanylation and 3-sulfenylation of indoles with dichalcogenides under mild conditions
Chen, Su-Qin,Wang, Qian-Mei,Xu, Ping-Chuan,Ge, Shao-Peng,Zhong, Ping,Zhang, Xiao-Hong
, p. 100 - 103 (2016/01/25)
A simple method was developed for the synthesis of 3-chalcogen indoles via iodine-promoted direct 3-selanyl- and 3-sulfenylation of indoles with dichalcogenides. The reaction was carried out smoothly in EtOH under air at room temperature, selectively givi
Iron-catalyzed sulfenylation of indoles with disulfides promoted by a catalytic amount of iodine
Fang, Xiao-Li,Tang, Ri-Yuan,Zhong, Ping,Li, Jin-Heng
experimental part, p. 4183 - 4189 (2011/02/28)
Selective sulfenylation of indoles with disulfides using iron(III) fluoride combined with iodine has been developed for the synthesis of sulfenylindoles. In the presence of iron(III) fluoride and iodine, a variety of disulfides underwent the reaction with indoles selectively to afford the corresponding sulfenylindoles in good to excellent yields. Moreover, reactions of indoles with 1,2-diphenyldiselane were also conducted under the same conditions, which smoothly afforded 3-selenylindoles in good yields. Georg Thieme Verlag Stuttgart - New York.
New arylthioindoles: Potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies
De Martino, Gabriella,Edler, Michael C.,La Regina, Giuseppe,Coluccia, Antonio,Barbera, Maria Chiara,Barrow, Denise,Nicholson, Robert I.,Chiosis, Gabriela,Brancale, Andrea,Hamel, Ernest,Artico, Marino,Silvestri, Romano
, p. 947 - 954 (2007/10/03)
Arylthioindoles (ATIs) that possess a 3-methoxyphenylthio or a 3,5-dimethoxyphenylthio moiety at position 2 of the indole ring were effective tubulin assembly inhibitors, but weak inhibitors of MCF-7 cell growth. ATIs bearing a 3-(3,4,5-trimethoxyphenyl)thio moiety were potent tubulin polymerization inhibitors, with IC50s in the 2.0 (35) to 4.5 (37) μM range. They also inhibited MCF-7 cell growth at nanomolar concentrations. The 3,4,5-trimethoxy substituted ATIs showed potencies comparable to those of the reference compounds colchicine and combretastatin A-4 in both tubulin assembly and cell growth inhibition assays. Dynamics simulation studies correlate well with the observed experimental data. Furthermore, from careful analysis of the biological and in silico data, we can now hypothesize a basic pharmacophore for this class of compounds.
ARYLTHIOINDOLE TUBULIN POLYMERIZATION INHIBITORS AND METHODS OF TREATING OR PREVENTING CANCER USING SAME
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Page/Page column 38-39, (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
3-substituted indole antiproliferative angiogenesis inhibitors
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, (2008/06/13)
3-Substituted indole carbohydrazides having the formula are useful for inhibiting angiogenesis and cell proliferation. Also disclosed are compositions which inhibit angiogenesis and cell proliferation and methods of inhibiting angiogenesis and cancer in a mammal.
A New Synthesis of 3-Arylthioindoles
Atkinson, Joseph G.,Hamel, Pierre,Girard, Yves
, p. 480 - 481 (2007/10/02)
The reaction of the anions of indoles with diaryl disulfides in dimethylformamide at room temperature gives the 3-arylthioindoles in 59-91percent yield.
