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Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 1 : Triazoles, triazolopyrimidines, triazinoindoles, quinoline hydrazones and arylpiperazines
- Llona-Minguez, Sabin (author)
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- Häggblad, Maria (author)
- Stockholms universitet,Institutionen för biokemi och biofysik,Science for Life Laboratory (SciLifeLab)
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- Martens, Ulf (author)
- Stockholms universitet,Institutionen för biokemi och biofysik,Science for Life Laboratory (SciLifeLab)
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- Throup, Adam (author)
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- (creator_code:org_t)
- Elsevier BV, 2017
- 2017
- English.
- In: Bioorganic & Medicinal Chemistry Letters. - : Elsevier BV. - 0960-894X .- 1464-3405. ; 27:16, s. 3897-3904
- Journal article (peer-reviewed)
Abstract
Subject headings
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- A high-throughput screening campaign using a commercial compound library (ChemBridge DiverSET) revealed diverse chemotypes as inhibitors of the human dCTP pyrophosphatase 1 (dCTPase). Triazole, triazolopyrimidine, triazinoindole, quinoline hydrazone and arylpiperazine hits were clustered, confirmed by IC50 determinations, and their preliminary structure-activity-relationships (SAR) and ligand efficiency scores are discussed in this letter.
Subject headings
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
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- ref (subject category)
- art (subject category)
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- Lundgren, Bo
- Scobie, Martin
- Helleday, Thomas
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- Karolinska Institutet
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