4-iodo-6-phenylpyrimidine and Carcinoma--Non-Small-Cell-Lung

The homologous cytokines macrophage migration inhibitory factor (MIF) and d-dopachrome tautomerase (d-DT or MIF2) play key roles in cancers. Molecules binding to the MIF tautomerase active site interfere with its biological activity. In contrast, the lack of potent MIF2 inhibitors hinders the exploration of MIF2 as a drug target. In this work, screening of a focused compound collection enabled the identification of a MIF2 tautomerase inhibitor R110. Subsequent optimization provided inhibitor

Topics: Antineoplastic Agents; Binding Sites; Carcinoma, Non-Small-Cell Lung; Cell Culture Techniques; Cell Cycle Checkpoints; Cell Line, Tumor; Cell Proliferation; Drug Design; Extracellular Signal-Regulated MAP Kinases; Humans; Intramolecular Oxidoreductases; Kinetics; Lung Neoplasms; Macrophage Migration-Inhibitory Factors; Molecular Dynamics Simulation; Phosphorylation; Pyrimidinones; Structure-Activity Relationship