Ontology highlight
ABSTRACT:
SUBMITTER: Lainchbury M
PROVIDER: S-EPMC3506129 | biostudies-literature | 2012 Nov
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20121019 22
Inhibitors of checkpoint kinase 1 (CHK1) are of current interest as potential antitumor agents, but the most advanced inhibitor series reported to date are not orally bioavailable. A novel series of potent and orally bioavailable 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitrile CHK1 inhibitors was generated by hybridization of two lead scaffolds derived from fragment-based drug design and optimized for CHK1 potency and high selectivity using a cell-based assay cascade. Efficient in viv ...[more]