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A Facile Synthesis of Ligands for the von Hippel–Lindau E3 Ligase
Synthesis ( IF 2.6 ) Pub Date : 2020-05-27 , DOI: 10.1055/s-0040-1707400
Michael Gütschow 1 , Christian Steinebach 1 , Sabine Anna Voell 1 , Lan Phuong Vu 1 , Aleša Bricelj 2 , Izidor Sosič 2 , Gregor Schnakenburg 3
Affiliation  

The proteolysis-targeting chimeras (PROTACs) have become an integral part of different stages of drug discovery. This growing field, therefore, benefits from advancements in all segments of the design of these compounds. Herein, an efficient and optimized synthetic protocol to various von Hippel-Lindau (VHL) ligands is presented, which enables easy access to multigram quantities of these essential PROTAC building blocks. Moreover, the elaborated synthesis represents a straightforward approach to further explore the chemical space of VHL ligands.

中文翻译:

von Hippel–Lindau E3连接酶的配体的简便合成

靶向蛋白水解的嵌合体(PROTAC)已成为药物发现不同阶段的组成部分。因此,这个不断发展的领域得益于这些化合物设计各方面的进步。本文中,提出了针对各种冯·希佩尔·林道(VHL)配体的高效且优化的合成方案,该方案可轻松访问以克为单位的这些基本PROTAC构建基块。此外,详细的合成方法是进一步探索VHL配体的化学空间的直接方法。
更新日期:2020-05-27
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