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Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1
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Number of Authors: 20
2017 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 60, no 5, 2148-2154 p.Article in journal (Refereed) Published
Abstract [en]

The dCTP pyrophosphatase 1 (dCTPase) is involved in the regulation of the cellular dNTP pool and has been linked to cancer progression. Here we report on the discovery of a series of 3,6-disubstituted triazolothiadiazoles as potent dCTPase inhibitors. Compounds 16 and 18 display good correlation between enzymatic inhibition and target engagement, together with efficacy in a cellular synergy model, deeming them as a promising starting point for hit -to-lead development.

Place, publisher, year, edition, pages
2017. Vol. 60, no 5, 2148-2154 p.
National Category
Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy) Medicinal Chemistry
Identifiers
URN: urn:nbn:se:su:diva-141203DOI: 10.1021/acs.jmedchem.6b01786ISI: 000396296100037PubMedID: 28145708OAI: oai:DiVA.org:su-141203DiVA: diva2:1091949
Available from: 2017-04-28 Created: 2017-04-28 Last updated: 2017-04-28Bibliographically approved

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Martens, UlfLundgren, Bo
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Department of Biochemistry and BiophysicsScience for Life Laboratory (SciLifeLab)
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Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)Medicinal Chemistry

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