Synthesis and Preclinical Validation of Novel Indole Derivatives as a GPR17 Agonist for Glioblastoma Treatment
Phung Kim Phi Nguyen, Phuong L. Doan, Tatu Rimpiläinen, Saravanan Konda Mani, Akshaya Murugesan, Olli Yli‐Harja, Nuno R. Candeias, Meenakshisundaram Kandhavelu
Abstract
of 85 μM, whereas the known agonist MDL29,951 showed a negligible effect. Our findings suggest that the phenolic Mannich base could be a better GPR17 agonist than MDL29,951, and further uncovering their pharmacological properties could potentiate an inventive GBM treatment.
Topics & Concepts
ChemistryAgonistCytotoxicityCheminformaticsCombinatorial chemistryLigand (biochemistry)PharmacologyActivator (genetics)Indole testDrug discoveryStereochemistryReceptorIn vitroBiochemistryComputational chemistryMedicineReceptor Mechanisms and SignalingChemical Synthesis and AnalysisComputational Drug Discovery Methods