4-(Acetylamino)-N-[2-amino-5-(2-thienyl)phenyl]-benzamide

OTAVA Catalogue Number: 7070707091
CAS Registry Number: 849234-64-6
Purity: 97%+

Ref.:  Witter et al. Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2). Bioorganic & Medicinal Chemistry Letters (2008), 18, 726-731

Abstract: A class of biaryl benzamides was identified and optimized as selective HDAC1 & 2 inhibitors (SHI-1:2). These agents exhibit selectivity over class II HDACs 4-7, as well as class I HDACs 3 and 8; providing examples of selective HDAC inhibitors for the HDAC isoforms most closely assocd. with  cancer. The hypothesis for the increased selectivity is the binding of a pendant arom. group in the internal cavity of the HDAC1&2 enzymes. SAR development based on an initial lead led to a series of potent and selective inhibitors with reduced off-target activity and tumor growth inhibition activity in a HCT-116 xenograft model.