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Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 2: Pyridone- and pyrimidinone-derived systems
Stockholm University, Faculty of Science, Department of Biochemistry and Biophysics. Stockholm University, Science for Life Laboratory (SciLifeLab).
Stockholm University, Faculty of Science, Department of Biochemistry and Biophysics. Stockholm University, Science for Life Laboratory (SciLifeLab).
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Number of Authors: 12
2017 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1090-2120, Vol. 27, no 15, 3219-3225 p.Article in journal (Refereed) Published
Abstract [en]

Two screening campaigns using commercial (Chembridge DiverSET) and proprietary (Chemical Biology Consortium Sweden, CBCS) compound libraries, revealed a number of pyridone- and pyrimidinone-derived systems as inhibitors of the human dCTP pyrophosphatase 1 (dCTPase). In this letter, we present their preliminary structure-activity-relationships (SAR) and ligand efficiency scores (LE and LLE).

Place, publisher, year, edition, pages
2017. Vol. 27, no 15, 3219-3225 p.
Keyword [en]
DCTPP1, Nucleotide metabolism, Pyridone, Pyrimidone
National Category
Chemical Sciences Pharmacology and Toxicology
Identifiers
URN: urn:nbn:se:su:diva-145862DOI: 10.1016/j.bmcl.2017.06.039ISI: 000405106500002PubMedID: 28655422OAI: oai:DiVA.org:su-145862DiVA: diva2:1135514
Available from: 2017-08-23 Created: 2017-08-23 Last updated: 2017-08-23Bibliographically approved

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