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GAC inhibitors with a 4-hydroxypiperidine spacer: Requirements for potency

Allosteric inhibitors of glutaminase (GAC), such as BPTES, CB-839 and UPGL00019, have great promise as inhibitors of cancer cell growth, but potent inhibitors with drug-like qualities have been difficult to achieve. Here, a small library of GAC inhibitors based on the UPGL00019 core is described. Th...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: McDermott, Lee, Koes, David, Mohammed, Shabber, Iyer, Prema, Boby, Melissa, Balasubramanian, Venkatakrishnan, Geedy, Mackenzie, Katt, William, Cerione, Richard
Formato: Artigo
Idioma:Inglês
Publicado em: 2019
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6889173/
https://ncbi.nlm.nih.gov/pubmed/31474484
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2019.126632
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