Discovery of novel JAK2 and EGFR inhibitors from a series of thiazole-based chalcone derivatives
Kamonpan Sanachai, Thitinan Aiebchun, Panupong Mahalapbutr, Supaphorn Seetaha, Lueacha Tabtimmai, Phornphimon Maitarad, Iakovos Xenikakis, Athina Geronikaki, Kiattawee Choowongkomon, Thanyada Rungrotmongkol
Abstract
formed a hydrogen bond with Met769 at the hinge region, Lys721 near a glycine loop, and Asp831 at the activation loop of EGFR. Altogether, these potent thiazole derivatives, following Lipinski's rule of five, could likely be developed as a promising JAK2/EGFR targeted drug(s) for cancer therapy.
Topics & Concepts
ChalconeChemistryThiazoleEpidermal growth factor receptorT790MEGFR inhibitorsKinaseCytotoxicityCancer cellCancer researchGefitinibBiochemistryStereochemistryCancerBiologyIn vitroReceptorGeneticsCytokine Signaling Pathways and InteractionsSynthesis and biological activityFungal Plant Pathogen Control