Ontology highlight
ABSTRACT:
SUBMITTER: Purkey HE
PROVIDER: S-EPMC5066143 | biostudies-literature | 2016 Oct
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20160826 10
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 IC<sub>50</sub> in a MiaPaca2 cell line. Optimization of the series led to <b>29</b>, a potent cell active molecule (MiaPaca2 IC<sub>50</sub> = 0.67 μM) that also possessed good exposure when dosed orally to mice. ...[more]