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Synthesis of Flavonols and Assessment of Their Biological Activity as Anticancer Agents.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2024 Apr 28; Vol. 29 (9). Date of Electronic Publication: 2024 Apr 28. - Publication Year :
- 2024
-
Abstract
- A series of flavanols were synthesized to assess their biological activity against human non-small cell lung cancer cells (A549). Among the sixteen synthesized compounds, it was observed that compounds 6k (3.14 ± 0.29 µM) and 6l (0.46 ± 0.02 µM) exhibited higher potency compared to 5-fluorouracil (5-Fu, 4.98 ± 0.41 µM), a clinical anticancer drug which was used as a positive control. Moreover, compound 6l (4'-bromoflavonol) markedly induced apoptosis of A549 cells through the mitochondrial- and caspase-3-dependent pathways. Consequently, compound 6l might be developed as a candidate for treating or preventing lung cancer.
- Subjects :
- Humans
A549 Cells
Caspase 3 metabolism
Cell Proliferation drug effects
Structure-Activity Relationship
Molecular Structure
Fluorouracil pharmacology
Mitochondria drug effects
Mitochondria metabolism
Drug Screening Assays, Antitumor
Lung Neoplasms drug therapy
Lung Neoplasms pathology
Lung Neoplasms metabolism
Cell Line, Tumor
Flavonols pharmacology
Flavonols chemical synthesis
Flavonols chemistry
Antineoplastic Agents pharmacology
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Apoptosis drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 29
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 38731532
- Full Text :
- https://doi.org/10.3390/molecules29092041