Deng, Xiangping; Liu, Renbo; Li, Junjian; Li, Zhongli; Liu, Juan; Xiong, Runde; Lei, Xiaoyong; Zheng, Xing; Xie, Zhizhong; Tang, Guotao published the artcile< Design, synthesis, and preliminary biological evaluation of 3',4',5'-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents>, Quality Control of 22717-55-1, the main research area is trimethoxy flavonoid salicylate derivative antitumor tubulin mol docking.
According to the pharmacophore combination principle, a set of new 3′,4′,5′-trimethoxy flavonoid salicylate derivatives were designed, synthesized, and evaluated for biol. activity. The cytotoxicity evaluation revealed that compound 10v exhibited higher potency than 5-Fu against HCT-116 cells. Preliminary biol. activity studies showed that compound 10v could inhibit the colony formation and migration of HCT-116 cells. Besides, the Hoechst 33258 staining assay and flow cytometry revealed that treatment with compound 10v induced the apoptosis of HCT-116 cells in a concentration-dependent manner, while it had no effect on their cell cycle. The WB anal. suggested that HIF-1α, tubulin, HK-2, and PFK might be the potential pharmacophore targets of compound 10v. Tubulin was a potential drug target for compound 10v, which was explained by analyzing the crystal structure of compound 10v complexed with tubulin. These results indicated that compound 10v might be a promising anti-tumor agent candidate, deserving further optimization and evaluation.
New Journal of Chemistry published new progress about Antitumor agents. 22717-55-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Quality Control of 22717-55-1.
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Chlorides – an overview | ScienceDirect Topics