Isoquinoline thiosemicarbazone displays potent anticancer activity with <i>in vivo</i> efficacy against aggressive leukemias
Daniel L. Sun, Soumya Poddar, Roy D. Pan, Ethan W. Rosser, Evan R. Abt, Juno Van Valkenburgh, Thuc Le, Vincent Lok, Selena Hernandez, Janet Song, Joanna Li, Aneta Turlik, Xiaohong Chen, Chi‐An Cheng, Wei Chen, Christine E. Mona, Andreea D. Stuparu, Laurent Vergnes, Karen Reue, Robert Damoiseaux, Jeffrey I. Zink, Johannes Czernin, Timothy R. Donahue, K. N. Houk, Michael E. Jung, Caius G. Radu
Abstract
Potent α-N-heterocyclic carboxaldehyde thiosemicarbazone (HCT) antiproliferatives were synthesized through iterative rounds of methylation and fluorination modifications, with anticancer activities being potentiated by physiological levels of copper.
Topics & Concepts
In vivoChemistryDNA damagePharmacologyCancer researchReactive oxygen speciesBiochemistryStereochemistryBiologyDNABiotechnologyMetal complexes synthesis and propertiesMetal-Organic Frameworks: Synthesis and ApplicationsDrug Transport and Resistance Mechanisms