Epigallocatechin gallate compound as well as preparation method and application thereof

• Main Authors: CHE XU, LEE HYUNG-YOON, LI HAIBO, XIAO HENG, YAO YANGRONG, LUO FAZENG
• Format: Patent
• Language: Chinese; English
• Published: 26.05.2023
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention relates to the technical field of drug synthesis, provides an epigallocatechin gallate compound, a preparation method thereof and application of the epigallocatechin gallate compound in antitumor drugs, and aims to solve the problems that EGCG (epigallocatechin gallate) contains a large number of phenolic hydroxyl groups in the structure, is unstable in property, easy to oxidize and denature, poor in fat solubility, short in holding time, to-be-improved in action intensity and the like. Therefore, a compound with stable chemical properties and better activity is obtained by modifying and optimizing a lipidation structure of EGCG, exploring and optimizing different reaction reagents, reagent molar ratios, solvents, reaction temperatures and reaction time and modifying specific sites. The preferable modified compound F4 shows a better anti-tumor activity effect than that of a raw material EGCG, and can kill cancer cells by inhibiting an MDM2 protein mediated P53-MDM2 pathway, inducing P53 mediated