Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor
Jo Waaler, Ruben G.G. Leenders, Sven T. Sowa, Shoshy Alam Brinch, Max Lycke, Piotr Nieczypor, Sjoerd Aertssen, Sudarshan Murthy, Albert Galera‐Prat, Eddy Damen, Anita Wegert, Marc Nazaré, L. Lehtiö, Stefan Krauß
Abstract
shows a favorable ADME profile, including improved Caco-2 permeability and oral bioavailability in mice, and exhibits antiproliferative efficacy in the colon cancer cell line COLO 320DM
Topics & Concepts
ChemistryWnt signaling pathwayADMELead compoundVirtual screeningLinkerTriazoleIC50Docking (animal)BiochemistryDrug discoveryPharmacologyIn vitroStereochemistrySignal transductionBiologyComputer scienceOperating systemMedicineOrganic chemistryNursingWnt/β-catenin signaling in development and cancerCancer-related gene regulationHippo pathway signaling and YAP/TAZ