Methyl ester of N-[[4-[[[2-amino-5-(2-thienyl)phenyl]amino]carbonyl]phenyl]methyl]-carbamic acid
OTAVAchemicals Catalogue Number: 7070707089
CAS Registry Number: 1013330-84-1
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.