| Literature DB >> 28145708 |
Sabin Llona-Minguez1, Andreas Höglund1, Elisee Wiita1, Ingrid Almlöf1, André Mateus2, José Manuel Calderón-Montaño1, Cindy Cazares-Körner1, Evert Homan1, Olga Loseva1, Pawel Baranczewski1,2, Ann-Sofie Jemth1, Maria Häggblad3, Ulf Martens3, Bo Lundgren3, Per Artursson2, Thomas Lundbäck1,4, Annika Jenmalm Jensen1,4, Ulrika Warpman Berglund1, Martin Scobie1, Thomas Helleday1.
Abstract
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.Entities:
Mesh：
Substances：
Year: 2017 PMID： 28145708 DOI： 10.1021/acs.jmedchem.6b01786
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446