Encyclopedia

  • Discovery of novel quinazoline-2,4(1H,3H)-dione derivatives as potent PARP-2 selective inhibitors
  • Add time:07/18/2019         Source:sciencedirect.com

    The PARP-2 selective inhibitor is important for clarifying specific roles of PARP-2 in the pathophysiological process and developing desired drugs with reduced off-target side effects. In this work, a series of novel quinazoline-2,4(1H,3H)-dione derivatives was designed and synthesized to explore isoform selective PARP inhibitors. As a result, compound 11a (PARP-1 IC50 = 467 nM, PARP-2 IC50 = 11.5 nM, selectivity PARP-1/PARP-2 = 40.6) was disclosed as the most selective PARP-2 inhibitor with high potency to date. The binding features of compound 11a within PARP-1 and PARP-2 were investigated respectively to provide useful insights for the further construction of new isoform selective inhibitors of PARP-1 and PARP-2 by using CDOCKER program.

    We also recommend Trading Suppliers and Manufacturers of 3-Butyl-6-methyl-2,4(1H,3H)-pyrimidinedione (cas 1010-90-8). Pls Click Website Link as below: cas 1010-90-8 suppliers


    Prev:Reduced Pyridine nucleotide-dependent N-hydroxy amine oxidase and reductase activities of hepatic microsomes
    Next: The metabolism of metronidazole (1 -2′-hydroxyethyl-2-methyl-5-nitroimidazole))

About|Contact|Cas|Product Name|Molecular|Country|Encyclopedia

Message|New Cas|MSDS|Service|Advertisement|CAS DataBase|Article Data|Manufacturers | Chemical Catalog

©2008 LookChem.com,License: ICP

NO.:Zhejiang16009103

complaints:service@lookchem.com Desktop View