Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors
Christine Brotherton‐Pleiss, Peibin Yue, Yinsong Zhu, Kayo Nakamura, Weiliang Chen, Wen‐Zhen Fu, Casie S. Kubota, Jasmine Chen, Felix Alonso-Valenteen, Simoun Mikhael, Lali K. Medina‐Kauwe, Marcus A. Tius, Francisco Lopez‐Tapia, James Turkson
Abstract
of 0.9-1.9 μM, cell growth, and colony survival, and induced apoptosis while having relatively weaker effects on normal breast epithelial, MCF-10A or breast cancer, MCF-7 cells that do not harbor constitutively active STAT3.
Topics & Concepts
ChemistryAzetidineSmall moleculeStereochemistryCombinatorial chemistryMoleculeStructure–activity relationshipBiochemistryIn vitroOrganic chemistryQuinazolinone synthesis and applicationsSynthesis and biological activityCytokine Signaling Pathways and Interactions