Polucci, Paolo published the artcileAlkylsulfanyl-1,2,4-triazoles, a New Class of Allosteric Valosine Containing Protein Inhibitors. Synthesis and Structure-Activity Relationships, Recommanded Product: (4-(Methoxycarbamoyl)phenyl)boronic acid, the publication is Journal of Medicinal Chemistry (2013), 56(2), 437-450, database is CAplus and MEDLINE.
Valosine containing protein (VCP), also known as p97, is a member of AAA ATPase family that is involved in several biol. processes and plays a central role in the ubiquitin-mediated degradation of misfolded proteins. VCP is an ubiquitously expressed, highly abundant protein and has been found overexpressed in many tumor types, sometimes associated with poor prognosis. In this respect, VCP has recently received a great deal of attention as a potential new target for cancer therapy. In this paper, the discovery and structure-activity relationships of alkylsulfanyl-1,2,4-triazoles, a new class of potent, allosteric VCP inhibitors, are described. Medicinal chem. manipulation of 3-(isopropylthio)-5-(phenoxymethyl)-4-phenyl-1,2,4-triazole, identified via HTS, led to the discovery of potent and selective inhibitors with submicromolar activity in cells and clear mechanism of action at consistent doses. This represents a first step toward a new class of potential anticancer agents.
Journal of Medicinal Chemistry published new progress about 850568-17-1. 850568-17-1 belongs to alcohols-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids, name is (4-(Methoxycarbamoyl)phenyl)boronic acid, and the molecular formula is C8H10BNO4, Recommanded Product: (4-(Methoxycarbamoyl)phenyl)boronic acid.
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