28837-78-7Relevant academic research and scientific papers
Detailed structure-activity relationship of indolecarboxamides as H 4 receptor ligands
Engelhardt, Harald,De Esch, Iwan J.P.,Kuhn, Daniel,Smits, Rogier A.,Zuiderveld, Obbe P.,Dobler, Julia,Mayer, Moriz,Lips, Sebastian,Arnhof, Heribert,Scharn, Dirk,Haaksma, Eric E.J.,Leurs, Rob
experimental part, p. 660 - 668 (2012/09/07)
A series of 76 derivatives of the indolecarboxamide 1 were synthesized, which allows a detailed SAR investigation of this well known scaffold. The data enable the definition of a predictive QSAR model which identifies several compounds with an activity comparable to 1. A selection of these new H 4R antagonists was synthesized and a comparison of predicted and measured values demonstrates the robustness of the model (47-55). In addition to the H4-receptor activity general CMC and DMPK properties were investigated. Some of the new analogs are not only excellently soluble, but display a significantly increased half-life in mouse liver microsomes as well. These properties qualify these compounds as a possible new standard for future in vivo studies (e.g 51, 52 and 55). Moreover, the current studies also provide valuable information on the potential receptor ligand interactions between the indolcarboxamides and the H4R protein.
3-SUBSTITUTED-1H-INDOLE, 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
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Page/Page column 103, (2010/04/06)
The invention relates to 3-substituted-1H-indole, 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula (I): or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
SUBSTITUTED INDOLES WITH SEROTONIN RECEPTOR AFFINITY, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page 28, (2010/02/09)
The present invention relates to the compounds represented by general formula (I) as shown below.
The first potent and selective non-imidazole human histamine H4 receptor antagonists
Jablonowski, Jill A.,Grice, Cheryl A.,Chai, Wenying,Dvorak, Curt A.,Venable, Jennifer D.,Kwok, Annette K.,Ly, Kiev S.,Wei, Jianmei,Baker, Sherry M.,Desai, Pragnya J.,Jiang, Wen,Wilson, Sandy J.,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 3957 - 3960 (2007/10/03)
Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.
Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents
Mahboobi,Pongratz,Hufsky,Hockemeyer,Frieser,Lyssenko,Paper,Bürgermeister,B?hmer,Fiebig,Burger,Baasner,Beckers
, p. 4535 - 4553 (2007/10/03)
A new class of simple synthetic antimitotic compounds based on 2-aroylindoles was discovered. (5-Methoxy-1H-2-indolyl)-phenylmethanone (1) as well as analogous 3-fluorophenyl- (36) and 3-methoxyphenyl (3) derivatives displayed high cytotoxicity of IC
