445490-65-3Relevant academic research and scientific papers
Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies
La Regina, Giuseppe,Edler, Michael C.,Brancale, Andrea,Kandil, Sahar,Coluccia, Antonio,Piscitelli, Francesco,Hamel, Ernest,De Martino, Gabriella,Matesanz, Ruth,Díaz, José Fernando,Scovassi, Anna Ivana,Prosperi, Ennio,Lavecchia, Antonio,Novellino, Ettore,Artico, Marino,Silvestri, Romano
, p. 2865 - 2874 (2008/02/08)
The new arylthioindole (ATI) derivatives 10, 14-18, and 21-24, which bear a halogen atom or a small size ether group at position 5 of the indole moiety, were compared with the reference compounds colchicine and combretastatin A-4 for biological activity. Derivatives 10, 11, 16, and 21-24 inhibited MCF-7 cell growth with IC50 values 2/M phase at 24 h, and at 48 h, 26% of the cells were hyperploid. Molecular modeling studies showed that, despite the absence of the ester moiety present in the previously examined analogues, most of the compounds bind in the colchicine site in the same orientation as the previously studied ATIs. Binding to β-tubulin involved formation of a hydrogen bond between the indole and Thr179 and positioning of the trimethoxy phenyl group in a hydrophobic pocket near Cys241.
Non-peptidic αvβ3 antagonists containing indol-1-yl propionic acids
Leonard, Kristi,Pan, Wenxi,Anaclerio, Beth,Gushue, Joan M.,Guo, Zihong,DesJarlais, Renee L.,Chaikin, Marge A.,Lattanze, Jennifer,Crysler, Carl,Manthey, Carl L.,Tomczuk, Bruce E.,Marugan, Juan Jose
, p. 2679 - 2684 (2007/10/03)
We describe the synthesis and structure/activity relationship of RGD mimetics that are potent inhibitors of the integrin αvβ 3. Indol-1-yl propionic acids containing a variety of basic moieties at the 5-position, as well as substitutions alpha and beta to the carboxy terminus were synthesized and evaluated. Novel compounds with improved potency have been identified.
Substituted indoles and their use as integrin antagonists
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, (2008/06/13)
The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
