التفاصيل البيبلوغرافية
| العنوان: |
Design, synthesis and activity evaluation of quinolinone derivatives as EZH2 inhibitors. |
| المؤلفون: |
Cai, Jin1 (AUTHOR) caijin@seu.edu.cn, You, Haoyuan1 (AUTHOR), Qin, Xintong1 (AUTHOR), Wang, Yuhong1 (AUTHOR), Li, Wei1 (AUTHOR) |
| المصدر: |
Bioorganic & Medicinal Chemistry Letters. Jun2024, Vol. 105, pN.PAG-N.PAG. 1p. |
| مصطلحات موضوعية: |
*LEAD compounds, *HISTONE methylation, *HELA cells, *LYSINE, *APOPTOSIS |
| مستخلص: |
[Display omitted] The enhancer of zeste homologue 2 (EZH2) is the core catalytic subunit of polycomb repressive complex 2, which catalyzes lysine 27 methylation of histone H3. Herein, a series of quinolinone derivatives were designed and synthesized based on the structure of Tazemetostat as the lead compound. Compound 9l (EZH2WT IC 50 = 0.94 nM) showed stronger antiproliferative activity in HeLa cells than the lead compound. Moreover, compound 9e (EZH2WT IC 50 = 1.01 nM) significantly inhibited the proliferation and induced apoptosis in A549 cells. [ABSTRACT FROM AUTHOR] |
| قاعدة البيانات: |
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