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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.

SUBMITTER: Green AI 

PROVIDER: S-EPMC8528209 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature

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Photochemical synthesis of an epigenetic focused tetrahydroquinoline library.

Green Adam I AI   Burslem George M GM  

RSC medicinal chemistry 20210825 10


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 (<i>e.g.</i>, kinases) resulting in low hit rates for epigenetic targets. Here we describe the design and synthesis of a compound co  ...[more]

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