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Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 2: Pyridone- and pyrimidinone-derived systems.
Llona-Minguez, Sabin; Häggblad, Maria; Martens, Ulf; Johansson, Lars; Sigmundsson, Kristmundur; Lundbäck, Thomas; Loseva, Olga; Jemth, Ann-Sofie; Lundgren, Bo; Jensen, Annika Jenmalm; Scobie, Martin; Helleday, Thomas.
  • Llona-Minguez S; Department of Medical Biochemistry and Biophysics, Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Karolinska Institutet, 17121 Stockholm, Sweden. Electronic address: sabin.llona.minguez@scilifelab.se.
  • Häggblad M; RNAi Cell Screening Facility, Department of Biochemistry and Biophysics, Science for Life Laboratory, Stockholm University, S-10691 Stockholm, Sweden.
  • Martens U; RNAi Cell Screening Facility, Department of Biochemistry and Biophysics, Science for Life Laboratory, Stockholm University, S-10691 Stockholm, Sweden.
  • Johansson L; Chemical Biology Consortium Sweden, Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
  • Sigmundsson K; Chemical Biology Consortium Sweden, Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
  • Lundbäck T; Chemical Biology Consortium Sweden, Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
  • Loseva O; Department of Medical Biochemistry and Biophysics, Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Karolinska Institutet, 17121 Stockholm, Sweden.
  • Jemth AS; Department of Medical Biochemistry and Biophysics, Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Karolinska Institutet, 17121 Stockholm, Sweden.
  • Lundgren B; RNAi Cell Screening Facility, Department of Biochemistry and Biophysics, Science for Life Laboratory, Stockholm University, S-10691 Stockholm, Sweden.
  • Jensen AJ; Chemical Biology Consortium Sweden, Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
  • Scobie M; Department of Medical Biochemistry and Biophysics, Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Karolinska Institutet, 17121 Stockholm, Sweden.
  • Helleday T; Department of Medical Biochemistry and Biophysics, Science for Life Laboratory, Division of Translational Medicine and Chemical Biology, Karolinska Institutet, 17121 Stockholm, Sweden. Electronic address: thomas.helleday@scilifelab.se.
Bioorg Med Chem Lett ; 27(15): 3219-3225, 2017 08 01.
Article en En | MEDLINE | ID: mdl-28655422
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).
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piridonas / Pirimidinonas / Pirofosfatasas / Inhibidores Enzimáticos Límite: Humans Idioma: En Año: 2017 Tipo del documento: Article
Texto completo
Imprimir
XML
PubMed Links
Search on Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piridonas / Pirimidinonas / Pirofosfatasas / Inhibidores Enzimáticos Límite: Humans Idioma: En Año: 2017 Tipo del documento: Article