57479-70-6Relevant articles and documents
Design, synthesis, and preliminary biological evaluation of 3′,4′,5′-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents
Deng, Xiangping,Liu, Renbo,Li, Junjian,Li, Zhongli,Liu, Juan,Xiong, Runde,Lei, Xiaoyong,Zheng, Xing,Xie, Zhizhong,Tang, Guotao
, p. 1874 - 1884 (2019/01/28)
According to the pharmacophore combination principle, a set of new 3′,4′,5′-trimethoxy flavonoid salicylate derivatives were designed, synthesized, and evaluated for biological activity. The cytotoxicity evaluation revealed that compound 10v exhibited higher potency than 5-Fu against HCT-116 cells. Preliminary biological 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 analysis 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.
Design, synthesis and biological evaluation of flavonoid salicylate derivatives as potential anti-tumor agents
Deng, Xiangping,Wang, Zhe,Liu, Juan,Xiong, Shujuan,Xiong, Runde,Cao, Xuan,Chen, Yanming,Zheng, Xing,Tang, Guotao
, p. 38171 - 38178 (2017/08/16)
A series of flavonoid salicylate derivatives containing trimethoxybenzene and a series of chrysin salicylate derivatives were synthesized for use as anti-tumor agents, and evaluated for antiproliferative activity using three human tumor cells: MCF-7 (breast carcinoma cells), HepG2 (liver carcinoma cells), MGC-803 (gastric carcinoma cells) and the mice tumor cells MFC (forestomach carcinoma cells). A substituent group of a suitable size and the trimethoxybenzene had a certain influence on the bioactivity of the flavonoid salicylate derivatives. Compound 2 and its salicylate derivatives 7a-7g containing the trimethoxybenzene exhibited more antiproliferative activity. Among them, compound 7g displayed the most potent antiproliferative activity against MGC-803 cells and MFC cells with the concentration causing 50% inhibition of cell growth (IC50) values of 11.05 ± 1.58 μM and 13.73 ± 2.04 μM, respectively. The flow cytometry results showed that compound 7g caused the cell cycle to be arrested in the G0/G1 phase and induced apoptosis of MFC cells in a dose-dependent manner. Furthermore, compound 7g showed good anti-tumor activity in vivo. These results suggested that compound 7g could be a new, potent anti-tumor candidate which should be optimized and evaluated further.
Meta-sulfonamido-benzamides
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, (2008/06/13)
Meta-sulfonamido-benzamide derivatives of the formula: STR1 [wherein R is a hydrogen atom or a lower alkyl, cyano, or lower alkanesulfonyl group; R1 is a lower alkyl, phenyl, amino, lower alkylamino, di(lower)alkylamino, or C4 -C5 alkyleneamino group; R2 is a hydrogen or halogen atom or a lower alkyl, di(lower)alkylamino, or lower alkoxy group; R3 is a hydrogen atom or a methyl or methoxy group; R4 is a hydrogen or halogen atom; R5 is a lower alkyl, lower alkenyl, C3 -C6 cycloalkyl, benzyl, or halogenobenzyl group; and n is 1 or zero] or their acid addition salts, showing pharmacological activity such as anti-emetic or psychotropic activity, are provided via several routes.