Ontology highlight
ABSTRACT:
SUBMITTER: Rai G
PROVIDER: S-EPMC5894102 | biostudies-literature | 2017 Nov
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20171109 22
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 multiparameter optimization enabled the development of compounds with potent enzymatic and cell-based inhibition of LDH enzymatic activity. Lead compounds such as 63 exhibit low nM inhibition of both LDHA and LDHB, submicrom ...[more]