Autor: |
Lee Apostle Mcdermott, Tianyi Yang, Richard A. Cerione, Lawrence Vernetti, William P. Katt, Jason W. O'Neill, Prema Iyer, Dylan J. Drakes, Michael Fioravanti, Melissa Boby, Jingran Sun, Qingqiu Huang, Shawn Rimer, Liwei Wang |
Jazyk: |
angličtina |
Rok vydání: |
2016 |
Předmět: |
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Popis: |
A novel set of GAC (kidney glutaminase isoform C) inhibitors able to inhibit the enzymatic activity of GAC and the growth of the triple negative MDA-MB-231 breast cancer cells with low nanomolar potency is described. Compounds in this series have a reduced number of rotatable bonds, improved C log Ps, microsomal stability and ligand efficiency when compared to the leading GAC inhibitors BPTES and CB-839. Property improvements were achieved by the replacement of the flexible n-diethylthio or the n-butyl moiety present in the leading inhibitors by heteroatom substituted heterocycloalkanes. |
Databáze: |
OpenAIRE |
Externí odkaz: |
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