Structure–Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer
Veronika F.S. Pape, Roberta Palkó, Szilárd Tóth, Miklós J. Szabó, Judit Sessler, György Dormán, Éva A. Enyedy, Tibor Soós, István Szatmári, Gergely Szakács
Abstract
values of the donor atom moieties, indicating that protonation and metal chelation are important factors modulating the MDR-selective anticancer activity of the studied compounds. Our results identify structural requirements increasing MDR-selective anticancer activity, providing guidelines for the development of more effective anticancer chelators targeting MDR cancer.
Topics & Concepts
ChemistryMannich baseMoietyMultiple drug resistanceCombinatorial chemistry8-HydroxyquinolineCytotoxicityProtonationStereochemistryCancer cellChelationChemical spaceCancerPharmacologyIn vitroBiochemistryOrganic chemistryDrug discoveryAntibioticsInternal medicineMedicineIonDrug Transport and Resistance MechanismsCancer therapeutics and mechanismsMetal complexes synthesis and properties