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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Vydáno v:J Med Chem
Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2017
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Article
On-line přístup: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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