mdl29-951 has been researched along with Astrocytoma* in 1 studies
1 other study(ies) available for mdl29-951 and Astrocytoma
| Article | Year |
|---|---|
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
The orphan receptor GPR17 may be a novel drug target for inflammatory diseases. 3-(2-Carboxyethyl)-4,6-dichloro-1 H-indole-2-carboxylic acid (MDL29,951, 1) was previously identified as a moderately potent GPR17 agonist. In the present study, we investigated the structure-activity relationships (SARs) of 1. Substitution of the indole 1-, 5-, or 7-position was detrimental. Only small substituents were tolerated in the 4-position while the 6-position accommodated large lipophilic residues. Among the most potent compounds were 3-(2-carboxyethyl)-1 H-indole-2-carboxylic acid derivatives containing the following substituents: 6-phenoxy (26, PSB-1737, EC Topics: Animals; Antineoplastic Agents; Astrocytoma; Calcium; Humans; Indoles; Models, Molecular; Molecular Structure; Protein Conformation; Rats; Receptors, G-Protein-Coupled; Structure-Activity Relationship; Tumor Cells, Cultured | 2018 |