Design, synthesis, and biological evaluation of a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon modulators was written by Liu, Yilin;Song, Yuming;Xu, Yingju;Jiang, Meixu;Lu, Haibin. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2022.Quality Control of 2-Chloro-6-nitrobenzoic acid This article mentions the following:
In the current study, we designed and synthesized a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon (CRBN) modulators. The results of the CCK8 assay revealed potent antiproliferative activity for the selected compound against NCI-H929 (IC50=2.25 μM) and U239 (IC50=5.86 μM) cell lines. Compound also can inhibit the TNF-α level (IC50=0.76 μM) in LPS stimulated PMBC and showed nearly no toxicity to this normal human cell line. The TR-FRET assay showed compound having potent inhibitory activity against CRBN (IC50=4.83 μM), and the docking study confirmed a nice fitting of into the active sites of CRBN. Further biol. studies revealed compound can increase the apoptotic events, arrest the NCI-H929 cells at G0/G1 cell cycle, and induce the ubiquitination degradation of IKZF1 and IKZF3 proteins by CRL4CRBN. These preliminary results suggested that compound could serve as a potential antitumor drug and worthy of further investigation. In the experiment, the researchers used many compounds, for example, 2-Chloro-6-nitrobenzoic acid (cas: 5344-49-0Quality Control of 2-Chloro-6-nitrobenzoic acid).
2-Chloro-6-nitrobenzoic acid (cas: 5344-49-0) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Quality Control of 2-Chloro-6-nitrobenzoic acid
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics