Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice
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https://figshare.com/articles/dataset/Cell_Active_Hydroxylactam_Inhibitors_of_Human_Lactate_Dehydrogenase_with_Oral_Bioavailability_in_Mice/3807312
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资源简介：
A series
of trisubstituted hydroxylactams was identified as potent
enzymatic and cellular inhibitors of human lactate dehydrogenase A.
Utilizing structure-based design and physical property optimization,
multiple inhibitors were discovered with <10 μM lactate IC50 in a MiaPaca2 cell line. Optimization of the series led
to 29, a potent cell active molecule (MiaPaca2 IC50 = 0.67 μM) that also possessed good exposure when
dosed orally to mice.
创建时间：
2016-10-07
