Novel Aryl-Substituted Pyrimidones as Inhibitors of 3-Mercaptopyruvate Sulfurtransferase with Antiproliferative Efficacy in Colon Cancer.
作者： Emmanuel Mikros , Vassilios Myrianthopoulos , Christian G Bochet , Csaba Szabo , Sofia Vasilakaki
DOI: 10.1021/ACS.JMEDCHEM.1C00260
关键词:
摘要: The enzyme 3-mercaptopyruvate sulfurtransferase (3-MST) is one of the more recently identified mammalian sources of H2S. A recent study identified several novel 3-MST inhibitors with micromolar potency. Among those,(2-[(4-hydroxy-6-methylpyrimidin-2-yl) sulfanyl]-1-(naphthalen-1-yl) ethan-1-one) or HMPSNE was found to be the most potent and selective. We now took the central core of this compound and modified the pyrimidone and the arylketone sides independently. A 63-compound library was synthesized; compounds …
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