10501-17-4Relevant articles and documents
INDOLOPYRIDINES AS INHIBITORS OF THE KINESIN SPINDLE PROTEIN (EG5 )
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Page/Page column 81, (2009/04/25)
Compounds of formula (I), in which R1, R2, R3 and R4 have the meanings indicated in the description, are effective Eg5-inhibiting compounds with anti-proliferative and/or apoptosis inducing activity.
TETRACYCLIC INDOLOPYRIDINES AS EG5 INHIBITORS
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Page/Page column 78, (2009/04/25)
Compounds of a certain formula (I), in which R1, R2, R3 and R4 have the meanings indicated in the description, are effective Eg5-inhibiting compounds with anti-proliferative and/or apoptosis inducing activity.
Solid state structure by X-ray and 13C CP/MAS NMR of new 5,5′-diethoxy-3,3′-methanediyl-bis-indole
Rasztawicka, Magdalena,Wolska, Irena,Maciejewska, Dorota
, p. 174 - 179 (2007/10/03)
5,5′-Diethoxy-3,3′-methanediyl-bis-indole 1 was synthesized by novel protocol and its solid state structure was analyzed using X-ray diffraction and 13C CP/MAS NMR methods. Double resonances were observed in the spectrum of 1, and different str
INDOLOPYRIDINES AS EG5 KINESIN MODULATORS
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Page/Page column 123, (2008/06/13)
Compounds of a certain formula (I), in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.
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.
The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists.
Buchheit,Gamse,Giger,Hoyer,Klein,Kloeppner,Pfannkuche,Mattes
, p. 2331 - 2338 (2007/10/02)
A number of substituted indole carbazimidamides were prepared and evaluated as 5-HT4 receptor agonists by using the isolated field-stimulated guinea pig ileum preparation. Their selectivity for the 5-HT4 receptor was established by examining their affinity for other 5-HT receptors using radioligand-binding techniques. Several selective and highly potent full as well as partial agonists emerged from this study. For example, 1b,d were found to be the most potent, full 5-HT4 receptor agonist described so far (EC50 = 0.5 and 0.8 nM, respectively), being 6 and 4 times more potent than serotonin itself. On the other hand, 5b and 1h appeared as partial 5-HT4 receptor agonists in the nonstimulated guinea pig ileum preparation with potencies, evaluated against serotonin action, respectively similar (5b, Ki = 12 nM) to and 300-fold higher (1h, Ki = 0.04 nM) than serotonin.
