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Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1
Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden..
Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden.;Sprint BioScience AB, Huddinge, Sweden..
Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden..
Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden..
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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
AMER CHEMICAL SOC , 2017. Vol. 60, no 5, 2148-2154 p.
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-319535DOI: 10.1021/acsjmedchem.6b01786ISI: 000396296100037PubMedID: 28145708OAI: oai:DiVA.org:uu-319535DiVA: diva2:1087255
Funder
Knut and Alice Wallenberg FoundationSwedish Research CouncilEU, European Research CouncilGöran Gustafsson Foundation for promotion of scientific research at Uppala University and Royal Institute of TechnologySwedish Cancer SocietySwedish Childhood Cancer FoundationTorsten Söderbergs stiftelseRagnar Söderbergs stiftelse
Available from: 2017-04-06 Created: 2017-04-06 Last updated: 2017-04-06Bibliographically approved

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Mateus, AndréBaranczewski, PawelArtursson, Per
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