93534-64-6Relevant academic research and scientific papers
Design synthesis and evaluation of novel aldose reductase inhibitors: The case of indolyl–sulfonyl–phenols
Koutsopoulos, Konstantinos,Lavrentaki, Vasiliki,Antoniou, Ioakeim,Kousaxidis, Antonios,Lefkopoulou, Matina,Tsantili-Kakoulidou, Anna,Kovacikova, Lucia,Stefek, Milan,Nicolaou, Ioannis
, (2020)
Therapeutic interventions with aldose reductase inhibitors appear to be a promising approach to major pathological conditions (i.e. neuropathy/angiopathy related to chronic hyperglycemia, chronic inflammation and cancer). Until now, the most potent aldose
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.
