Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl) benzamides
Bioorganic & medicinal chemistry letters, 2010•Elsevier
A series of N-(2-amino-5-substituted phenyl) benzamides (3–21) were designed,
synthesized and evaluated for their inhibition of HDAC2 and their cytotoxicity in HCT116
cancer cells. Multiple compounds from this series demonstrated time-dependent binding
kinetics that is rationalized using a co-complex crystal structure of HDAC2 and N-(4-
aminobiphenyl-3-yl) benzamide (6).
synthesized and evaluated for their inhibition of HDAC2 and their cytotoxicity in HCT116
cancer cells. Multiple compounds from this series demonstrated time-dependent binding
kinetics that is rationalized using a co-complex crystal structure of HDAC2 and N-(4-
aminobiphenyl-3-yl) benzamide (6).
A series of N-(2-amino-5-substituted phenyl)benzamides (3–21) were designed, synthesized and evaluated for their inhibition of HDAC2 and their cytotoxicity in HCT116 cancer cells. Multiple compounds from this series demonstrated time-dependent binding kinetics that is rationalized using a co-complex crystal structure of HDAC2 and N-(4-aminobiphenyl-3-yl)benzamide (6).
Elsevier