Ontology highlight
ABSTRACT:
SUBMITTER: Palacios DS
PROVIDER: S-EPMC6862340 | biostudies-literature | 2019 Nov
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20191010 11
Small molecules that inhibit the metabolic enzyme NAMPT have emerged as potential therapeutics in oncology. As part of our effort in this area, we took a scaffold morphing approach and identified 3-pyridyl azetidine ureas as a potent NAMPT inhibiting motif. We explored the SAR of this series, including 5 and 6 amino pyridines, using a convergent synthetic strategy. This lead optimization campaign yielded multiple compounds with excellent in vitro potency and good ADME properties that culminated ...[more]