Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 2: Pyridone- and pyrimidinone-derived systems

作者：Llona Minguez Sabin^*; Haggblad Maria; Martens Ulf; Johansson Lars; Sigmundsson Kristmundur; Lundback Thomas; Loseva Olga; Jemth Ann Sofie; Lundgren Bo; Jensen Annika Jenmalm; Scobie Martin; Helleday Thomas^*

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(15): 3219-3225.

DOI：10.1016/j.bmcl.2017.06.039

• DCTPP1
• Nucleotide metabolism
• Pyridone
• Pyrimidone

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).

• 出版日期2017-8-1