Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors-Reference-Cited by-同舟云学术

Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors

Published:2019 Issue:2 Volume:10 Page:263-267
ISSN:2040-2503
Container-title:MedChemComm
language:en
Short-container-title:Med. Chem. Commun.

Author:

Keeley A.¹²³⁴⁵,Ábrányi-Balogh P.¹²³⁴⁵^ORCID,Keserű G. M.¹²³⁴⁵^ORCID

Affiliation:

1. Medicinal Chemistry Research Group

2. Research Centre for Natural Sciences

3. Hungarian Academy of Sciences

4. H-1117 Budapest

5. Hungary

Abstract

A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads.

Funder

Országos Tudományos Kutatási Alapprogramok

H2020 Marie Skłodowska-Curie Actions

Magyar Tudományos Akadémia

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2019/MD/C8MD00327K

Reference14 articles.

1. Rings in Drugs

2. The influence of lead discovery strategies on the properties of drug candidates

3. Design Principles for Fragment Libraries: Maximizing the Value of Learnings from Pharma Fragment-Based Drug Discovery (FBDD) Programs for Use in Academia

4. The resurgence of covalent drugs

5. Targeted Covalent Inhibitors for Drug Design

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