Zhang, Bo published the artcileDiscovery of novel aminophosphonate derivatives containing pyrazole moiety as potential selective COX-2 inhibitors, Quality Control of 1468-83-3, the main research area is aminophosphonate preparation anticancer pyrazole inhibitor amidation human COX MSBAR; Aminophosphonate derivatives; Anti-cancer activity; Apoptosis induction; Cyclooxygenase 2; Mitochondrion-dependent pathway; Pyrazole moiety.
Cyclooxygenase is critical for maintaining physiol. functions, whereas overexpression of COX-2 was closely implicated in various cancers. In this study, a series of novel aminophosphonate derivatives containing pyrazole moiety were synthesized with their anti-cancer activity evaluated. In vitro assays of the target compounds showed that (I) displayed excellent COX-2 inhibitory activity against COX-2 (IC50 = 0.22 ± 0.04μM) and anti-proliferative activity against MCF-7 cell (IC50 = 4.37 ± 0.49μM). The apoptosis induction of compound I was confirmed by flow cytometry and polymerase chain reaction. Further investigation demonstrated that compound I induced apoptosis of MCF-7 cells through a mitochondrion-dependent pathway and involved cell-cycle arrest in G2 phase. Overall, these results provided some new insights into the design of therapeutic drugs for COX-2 inhibitors and indicated the connection between selective COX-2 inhibition and the anti-tumor activity.
Bioorganic Chemistry published new progress about Amidation. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Quality Control of 1468-83-3.
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem