Xie, Rui published the artcileDesign, synthesis and biological evaluation of novel hydroxamates and 2-aminobenzamides as potent histone deacetylase inhibitors and antitumor agents, Application of 4-(Phenoxymethyl)benzoic acid, the publication is European Journal of Medicinal Chemistry (2017), 1-12, database is CAplus and MEDLINE.
Many studies have indicated that histone deacetylase (HDAC) inhibitors are promising agents for the treatment of cancer. With the aim to search for novel potent HDAC inhibitors, two series of hydroxamates and 2-aminobenzamides 4-R1CH2C6H4CONHR2 [R1 = PhO, 4-HON:CMeC6H4O, R2 = OH; R1 = PhO, 4-MeOC6H4O, 5-bromo-2,3-dihydro-1H-indol-1-yl, etc., R2 = 2-H2NC6H4, 2-H2N-4-FC6H3] and (E)-4-R1CH2C6H4CH:CHCONHR2 [R1 = PhO, 2,3-dihydro-1H-indol-1-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl; R2 = OH, 2-H2NC6H4, 3-aminopyridin-4-yl] were designed and synthesized as HDAC inhibitors and antitumor agents. Those compounds were investigated for their HDAC enzymic inhibitory activities and in vitro anti-proliferation activities against diverse cancer cell line (A549, HepG2, MGC80-3 and HCT116). Most of the synthesized compounds displayed potent HDAC inhibitory activity and antiproliferative activity. In particular, the compound 4-R1CH2C6H4CONHR2 (R1 = 4-FC6H4O; R2 = 2-H2NC6H4) (I) was shown to have the most HDAC inhibitory activity (70.6% inhibition at 5 ¦ÌM) and antitumor activity with IC50 value of as low as 3.84 ¦ÌM against HepG2 human liver hepatocellular carcinoma cell line, more than 4.8-fold lower than CS055 and 5.9-fold lower than CI994. HDAC isoform selectivity assay indicated the compound I is a potent HDAC2 inhibitor. Docking study of I suggested that it bound tightly to the binding pocket of HDAC2. Further investigation showed that the compound I could inhibit the migration and colony formation of A549 cancer cells. Furthermore, this compound remarkably induced apoptosis and G2/M phase cell cycle arrest in A549 cancer cells. Those results indicated that the compound I could be a promising candidate for treatment of cancer.
European Journal of Medicinal Chemistry published new progress about 31719-76-3. 31719-76-3 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ether, name is 4-(Phenoxymethyl)benzoic acid, and the molecular formula is C40H35N7O8, Application of 4-(Phenoxymethyl)benzoic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia