Structure-based design and synthesis of a novel long-chain 4′′-alkyl ether derivative of EGCG as potent EGFR inhibitor: <i>in vitro</i> and <i>in silico</i> studies
Satyam Singh, Revathy Sahadevan, Rajarshi Roy, Mainak Biswas, Priya Ghosh, Parimal Kar, Avinash Sonawane, Sushabhan Sadhukhan
Abstract
Among the synthesized 4′′-alkyl EGCG derivatives, 4′′-C 14 EGCG inhibited EGF stimulated phosphorylation of EGFR and its downstream signaling pathways, ERK and Akt. 4′′-C 14 EGCG showed significantly improved stability than EGCG and induced apoptosis.
Topics & Concepts
ChemistryHeLaAutophosphorylationApoptosisDownregulation and upregulationCell culturePopulationMAPK/ERK pathwayBiochemistryIn vitroKinaseProtein kinase ABiologyMedicineEnvironmental healthGeneticsGeneHER2/EGFR in Cancer ResearchSynthesis and biological activityChemical Synthesis and Analysis