Saeed, Aamer published the artcileSynthesis, cytotoxicity and molecular modelling studies of new phenylcinnamide derivatives as potent inhibitors of cholinesterases, Application of (E)-3-(3-Nitrophenyl)acrylic acid, the publication is European Journal of Medicinal Chemistry (2014), 43-53, database is CAplus and MEDLINE.
The present study reports the synthesis of cinnamides I [R = 4-ClC6H4, 3-O2NC6H4, 2-F-6-ClC6H3, etc.] and their biol. activity as inhibitors of both cholinesterases and anticancer agents. Controlled inhibition of brain acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) may slow neurodegeneration in Alzheimer’s diseases (AD). The anticholinesterase activity of phenylcinnamide derivatives was determined against Elec. Eel acetylcholinesterase (EeAChE) and horse serum butyrylcholinesterase (hBChE) and some of the compounds appeared as moderately potent inhibitors of EeAChE and hBChE. Compound I [R = 2-(PhCH2O)C6H4] showed maximum activity against EeAChE with an IC50 0.29¡À0.21 ¦ÌM whereas I [R = 2-Cl-6-NO2C6H3] was proved to be the most potent inhibitor of hBChE having IC50 1.18¡À1.31 ¦ÌM. To better understand the enzyme-inhibitor interaction of the most active compounds toward cholinesterases, mol. modeling studies were carried out on high-resolution crystallog. structures. The anticancer effects of synthesized compounds were also evaluated against cancer cell line (lung carcinoma). The compounds may be useful leads for the design of a new class of anticancer drugs for the treatment of cancer and cholinesterase inhibitors for Alzheimer’s disease.
European Journal of Medicinal Chemistry published new progress about 1772-76-5. 1772-76-5 belongs to catalysis-chemistry, auxiliary class Benzenes, name is (E)-3-(3-Nitrophenyl)acrylic acid, and the molecular formula is C9H7NO4, Application of (E)-3-(3-Nitrophenyl)acrylic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia