Liu, Yilin; Song, Yuming; Xu, Yingju; Jiang, Meixu; Lu, Haibin published an article in 2022, the title of the article was 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.HPLC of Formula: 99-60-5 And the article contains the following content:
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. The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).HPLC of Formula: 99-60-5
The Article related to isoquinolinedione derivative synthesis cereblon modulator antitumor antiproliferative, anticancer, crbn, imids, nci-h929, Placeholder for records without volume info and other aspects.HPLC of Formula: 99-60-5
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