| Autor: |
Jung, Goni, Lee, Joo‐Youn, Park, Chi Hoon, Yoon, Eunyoung, Heo, Jung‐Nyoung |
| Zdroj: |
Bulletin of the Korean Chemical Society; March 2023, Vol. 44 Issue: 3 p213-221, 9p |
| Abstrakt: |
A novel series of benzo[6,7]oxepino[4,3,2‐cd]indol‐1(2H)‐one derivatives were synthesized via a one‐pot aldol condensation and SNAr reaction by coupling indolin‐2‐ones with 2‐fluorobenzaldehydes. In addition, molecular docking studies of the designed compound 2revealed strong hydrogen bonds in the hot binding pocket of Brd4. All compounds were evaluated for their enzymatic activity in Brd4 bromodomain inhibition. A novel series of benzo[6,7]oxepino[4,3,2‐cd]indol‐1(2H)‐one derivatives were synthesized via a one‐pot aldol condensation and SNAr reaction by coupling indolin‐2‐ones with 2‐fluorobenzaldehydes. In addition, molecular docking studies of the designed Compound 2revealed strong hydrogen bonds in the hot binding pocket of Brd4. All compounds were evaluated for their enzymatic activity in Brd4 bromodomain inhibition. |
| Databáze: |
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