Issue 10, 2021

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
01 ذو القعدة 1442
Accepted
16 محرم 1443
First published
17 محرم 1443

RSC Med. Chem., 2021,12, 1780-1786

Author version available

Photochemical synthesis of an epigenetic focused tetrahydroquinoline library

A. I. Green and G. M. Burslem, RSC Med. Chem., 2021, 12, 1780 DOI: 10.1039/D1MD00193K

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements