Photochemical synthesis of an epigenetic focused tetrahydroquinoline library

Abstract

Discovery of epigenetic chemical probes is an important area of research with potential to deliver drugs for a multitude of diseases. However, commercially available libraries frequently used in drug discovery campaigns contain molecules that are focused on a narrow range of chemical space primarily driven by ease of synthesis and previously targeted enzyme classes (e.g., kinases) resulting in low hit rates for epigenetic targets. Here we describe the design and synthesis of a compound collection that augments current screening collections by the inclusion of privileged isosteres for epigenetic targets.

Graphical abstract: Photochemical synthesis of an epigenetic focused tetrahydroquinoline library

Supplementary files

Article information

Article type
Research Article
Submitted
11 Jun 2021
Accepted
24 Aug 2021
First published
25 Aug 2021

RSC Med. Chem., 2021, Advance Article

Photochemical synthesis of an epigenetic focused tetrahydroquinoline library

A. I. Green and G. M. Burslem, RSC Med. Chem., 2021, Advance Article , DOI: 10.1039/D1MD00193K

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