Discovery of a Potential Multi-Target Anti-Tumor Agent via Structural Modification on Flavonoid
A series of flavonoid derivatives bearing trimethoxyphenyl and benzimidazole were designed, synthesized and evaluated as potential anti-tumor agents. Compound 5g showed remarkable inhibitory activity against SGC-7901, HGC-27 and MCF-7 (IC 50 values of 20.5 ± 5.93, 3.3 ± 2.53 and 16.6 ± 0.75 μM, resp...
Saved in:
Published in | Polycyclic aromatic compounds Vol. 43; no. 2; pp. 980 - 999 |
---|---|
Main Authors | , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Philadelphia
Taylor & Francis
07.02.2023
Taylor & Francis Ltd |
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | A series of flavonoid derivatives bearing trimethoxyphenyl and benzimidazole were designed, synthesized and evaluated as potential anti-tumor agents. Compound 5g showed remarkable inhibitory activity against SGC-7901, HGC-27 and MCF-7 (IC
50
values of 20.5 ± 5.93, 3.3 ± 2.53 and 16.6 ± 0.75 μM, respectively), and had great selectivity to cancer cells. The results of Hoechst 33258 staining and Annexin V-FITC/PI dual staining confirmed that compound 5 g induced apoptosis of the HGC-27 cells in a concentration-dependent manner. After treatment with compound 5 g, the expression of HIF-1α, VEGF and PKM2 were down-regulated, accompanied by weakened the levels of lactate. Further research revealed that compound 5 g could obviously inhibit tubulin assembly. In summary, compound 5 g possessed a promising potential for further development into anti-tumor drug candidates. |
---|---|
ISSN: | 1040-6638 1563-5333 |
DOI: | 10.1080/10406638.2021.2021251 |