10242-08-7Relevant articles and documents
Synthesis and AChE inhibitory activity of N-glycosyl benzofuran derivatives
Cao, Zhi-Ling,Liu, Shu-Hao,Liu, Wei-Wei,Liu, Xiu-Jian,Ren, Shu-Ting,Shi, Da-Hua,Wang, Lei,Wang, You-Xian,Wu, Yu-Ran
, p. 162 - 166 (2019)
Six N-glycosyl benzofuran derivatives were synthesized by the catalysis of organic bases and condensation agents. The benzofuran derivatives were obtained by the reaction of various salicylaldehydes in acetone, and then hydrolyzed to the corresponding carboxylic acids. Finally, the target compounds were synthesized by acylation and the reaction conditions were optimized. The acetylcholinesterase (AChE) inhibitory activity of the desired compounds was tested using Ellman's method. Most of the compounds showed acetylcholinesterase-inhibition activity; N-(2,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)benzofuran-2-carbxamide (5a) showed the best acetylcholinesterase inhibition, with an inhibitory rate of 84%.
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Tanaka
, p. 872 (1951)
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Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site
Kong, Ling-Yi,Leng, Jia-Fu,Lian, Bao-Ping,Shao, Yu-Ying,Xia, Yuan-Zheng,Yin, Yong
, (2020/02/11)
A novel series of shikonin-benzo[b]furan derivatives were designed and synthesized as tubulin polymerization inhibitors, and their biological activities were evaluated. Most compounds revealed the comparable anti-proliferation activities against the cancer cell lines to that of shikonin and simultaneously low cytotoxicity to non-cancer cells. Among them, compound 6c displayed powerful anti-cancer activity with the IC50 value of 0.18 μM against HT29 cells, which was significantly better than that of the reference drugs shikonin and CA-4. What's more, 6c could inhibit tubulin polymerization and compete with [3H] colchicine in binding to tubulin. Further biological studies depicted that 6c can induce cell apoptosis and cell mitochondria depolarize, regulate the expression of apoptosis related proteins in HT29 cells. Besides, 6c actuated the HT29 cell cycle arrest at G2/M phase, and influenced the expression of the cell-cycle related protein. Moreover, 6c displayed potent inhibition on cell migration and tube formation that contributes to the antiangiogenesis. These results prompt us to consider 6c as a potential tubulin polymerization inhibitor and is worthy for further study.
Benzocarbazoles five-membered unsaturated heterocyclic compound or its pharmaceutically acceptable salts and its preparation method, pharmaceutical composition and its application
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, (2016/10/08)
Provided in the present invention are an unsaturated 5-membered benzo-heterocyclic compound with the structure as shown in general formula I or pharmaceutical salts thereof, and a preparation method, a pharmaceutical composition and the use thereof. Experiments have shown that the compound of the present invention has the effects of upregulating the expression activity of bone morphogenetic protein BMP-2 and anti-osteoporosis in vivo, and also has the effect of improving SAMP6 mice osteoporosis symptoms. Activity tests in vitro have shown that the compound of the present invention shows an obvious upregulation effect on bone morphogenetic protein BMP-2.