HDAC degradation agent taking alkane or fatty acid as connecting chain as well as preparation method and application of HDAC degradation agent

• Main Authors: DU WENTING, LING JIANAN, WANG JIAN, LI JUN, ZENG XIAN-MING, XU SHENPENG, SHAO MEIQI, CHEN WENTIAN
• Format: Patent
• Language: Chinese; English
• Published: 30.06.2023
• 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 provides an HDAC degradation agent taking alkane or fatty acid as a connecting chain as well as a preparation method and application of the HDAC degradation agent, and relates to the technical field of medicines. The chemical structure of the HDAC degradation agent provided by the invention comprises a ubiquitin ligase E3 ligand and vorinostat, and the ubiquitin ligase E3 ligand and vorinostat take alkane or fatty acid as a connecting chain. A PROTAC molecule taking vorinostat as a target protein is designed and synthesized by utilizing a protein degradation strategy, and the PROTAC molecule has the potential of solving the problem of serious toxic and side effects of the current marketed drug vorinostat by remarkably reducing the dosage. According to the preparation method of the HDAC degradation agent, the used raw materials are simple, convenient and easy to obtain, the method is simple and convenient in step operation and high in yield, application of large instruments and equipment is not n