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

In the current study, we designed and synthesised 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 10a against NCI-H929 (IC 50 =2.25...

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Veröffentlicht in:	Journal of enzyme inhibition and medicinal chemistry 2022-12, Vol.37 (1), p.1715-1723
Hauptverfasser:	Liu, Yilin, Song, Yuming, Xu, Yingju, Jiang, Meixu, Lu, Haibin
Format:	Artikel
Sprache:	eng
Schlagworte:	Adaptor Proteins, Signal Transducing - metabolism Anticancer Antineoplastic Agents - pharmacology Apoptosis Cancer Cell cycle Cell Line, Tumor Cell lines Cell Proliferation CRBN Drug Screening Assays, Antitumor Fluorescence resonance energy transfer Growth factors Humans IMiDs Investigations Isoquinolines Lipopolysaccharides NCI-H929 Pharmacy Research Paper Structure-Activity Relationship Toxicity Tumor necrosis factor-TNF Tumor necrosis factor-α Ubiquitin-Protein Ligases - metabolism Ubiquitination
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