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Discovery and Optimization of potent, cell-active pyrazole-based inhibitors of Lactate Dehydrogenase (LDH)

We report the discovery and medicinal chemistry optimization of a novel series of pyrazole-based inhibitors of human lactate dehydrogenase (LDH). Utilization of a quantitative high-throughput screening paradigm facilitated hit identification while structure-based design and multi-parameter optimizat...

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Publicado no:J Med Chem
Main Authors: Rai, Ganesha, Brimacombe, Kyle R., Mott, Bryan T., Urban, Daniel J., Hu, Xin, Yang, Shyh-Ming, Lee, Tobie D., Cheff, Dorian M., Kouznetsova, Jennifer, Benavides, Gloria A., Pohida, Katie, Kuenstner, Eric J., Luci, Diane K., Lukacs, Christine M., Davies, Douglas R., Dranow, David M., Zhu, Hu, Sulikowski, Gary, Moore, William J., Stott, Gordon M., Flint, Andrew J., Hall, Matthew D., Darley-Usmar, Victor M., Neckers, Leonard M., Dang, Chi V., Waterson, Alex G., Simeonov, Anton, Jadhav, Ajit, Maloney, David J.
Formato: Artigo
Idioma:Inglês
Publicado em: 2017
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Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5894102/
https://ncbi.nlm.nih.gov/pubmed/29120638
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.7b00941
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