4'-substituted analogues of fisetin and their use in the treatment of cancer
4'-Substituted Fisetin analogues with ring-deactivating groups address the lack of clear cytotoxicity patterns by enhancing activity against lung cancer cells, inducing cell cycle arrest and apoptosis, making them effective chemotherapeutic candidates.
Patent Information
- Application Number
- GB2023008216
- Authority / Receiving Office
- GB · GB
- Patent Type
- Patents
- Current Assignee / Owner
- Priority Date
- 2020-11-30
- Filing Date
- 2021-11-30
- Publication Date
- 2025-08-13
- Estimated Expiration
- 2041-11-30
AI Technical Summary
There is a need to develop 4'-substituted analogues of Fisetin that exhibit enhanced cytotoxicity against epithelial cancer cells, particularly lung cancer cells, as existing studies have not established clear substitution patterns for improved cytotoxicity in flavonols.
Synthesis of Fisetin analogues with ring-deactivating groups at the 4'-position, such as -Br, -Cl, -CF3, and -SO2CH3, which enhance cytotoxicity by correlating with a positive para-Hammett constant, leading to compounds like 4'-bromo, 4'-chloro, and 4'-CF3 derivatives showing significant activity against lung cancer cell lines.
The 4'-substituted Fisetin analogues demonstrate enhanced cytotoxicity against lung cancer cell lines, inducing G2/M cell cycle arrest, apoptosis, and modulating key proteins, offering potential as chemotherapeutic agents.