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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Bibliografiset tiedot
Julkaisussa:J Med Chem
Päätekijät: 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.
Aineistotyyppi: Artigo
Kieli:Inglês
Julkaistu: 2017
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Article
Linkit: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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