Discovery of a Potential Multi-Target Anti-Tumor Agent via Structural Modification on Flavonoid. (7th February 2023)

• Record Type: Journal Article
• Authors: Deng, Xiangping; Zou, Yang; Liu, Renbo; Peng, Yijiao; Ouyang, Chenglin; Peng, Junmei; Lei, Xiaoyong; Xie, Zhizhong; Li, Chong; Tang, Guotao
• Is Part Of: Polycyclic aromatic compounds. Volume 43:Number 2(2023)
• Page Start: 980
• Page End: 999
• Publication Date: 2023-02-07
• Subjects: Synthesis -- flavonoid -- trimethoxyphenyl -- benzimidazole -- anti-tumor; Polycyclic aromatic compounds -- Periodicals; 547
• DOI: 10.1080/10406638.2021.2021251
• Languages: English
• ISSNs: 1040-6638

Abstract

Abstract: 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 (IC50 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. Graphical Abstract: UF0001