Ontology highlight
ABSTRACT:
SUBMITTER: Barlaam B
PROVIDER: S-EPMC6088353 | biostudies-literature | 2018 Aug
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20180713 8
We report the discovery of a novel series of 3-cinnoline carboxamides as highly potent and selective ataxia telangiectasia mutated (ATM) kinase inhibitors. Optimization of this series focusing on potency and physicochemical properties (especially permeability) led to the identification of compound <b>21</b>, a highly potent ATM inhibitor (ATM cell IC<sub>50</sub> 0.0028 μM) with excellent kinase selectivity and favorable physicochemical and pharmacokinetics properties. <i>In vivo</i>, <b>21</b> ...[more]