Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors

Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors

“…12 Extensive research has been conducted on the derivatization of the cap group, to optimize drug-target interactions. 12 Recently, we have initiated the search for moieties that would retain the zinc-binding properties and enzyme inhibitory activity of the hydroxamic acid group. In this Letter we report the attempts made to modify the ZBG-functionality of the 4-vinylbiphenyl scaffold.…”

“…1). 12 Extensive research has been conducted on the derivatization of the cap group, to optimize drug-target interactions. [12][13][14] http://dx.…”

Synthesis, molecular modeling, and biological evaluation of cinnamic acid metronidazole ester derivatives as novel anticancer agents

“…Particularly, cinnamic acid ester derivatives shown the potential antitumor activity. [20][21][22] In this study, we described the synthesis and the SAR of the novel series of cinnamic acid metronidazole ester derivatives, and the biological activity evaluation indicated that some of these compounds are potent inhibitors of EGFR and HER-2. Docking simulations were performed using the X-ray crystallographic structure of the EGFR in complex with an inhibitor to explore the binding modes of these compounds at the active site.…”

Synthesis and biological evaluation of hydroxycinnamic acid hydrazide derivatives as inducer of caspase-3

“…Particularly, the derivatives is considered to be promising anticancer drug due to its efficient induction of proliferation arrest and apoptosis in a variety of tumor cells [11e13]. A number of studies indicated that most of their pharmacological properties are considered to be due to their antioxidant action [14,15].…”