Ontology highlight
ABSTRACT:
SUBMITTER: Nathubhai A
PROVIDER: S-EPMC4027532 | biostudies-literature | 2013 Dec
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20131015 12
Tankyrases (TNKSs) are poly(ADP-ribose)polymerases (PARPs) that are overexpressed in several clinical cancers. They regulate elongation of telomeres, regulate the Wnt system, and are essential for the function of the mitotic spindle. A set of 2-arylquinazolin-4-ones has been designed and identified as potent and selective TNKS inhibitors, some being more potent and selective than the lead inhibitor XAV939, with IC50 = 3 nM vs. TNKS-2. Methyl was preferred at the 8-position and modest bulk at the ...[more]