國家衛生研究院 NHRI:Item 3990099045/8860
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    题名: Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes
    作者: Lee, HY;Chang, CY;Lai, MJ;Chuang, HY;Kuo, CC;Chang, CY;Chang, JY;Liou, JP
    贡献者: Institute of Biotechnology and Pharmaceutical Research;National Institute of Cancer Research
    摘要: This study reports the synthesis of a series of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes, which are potent antitubulin agents. Compound 13, (2-hydroxy-3,4,5-trimethoxyphenyl)-(6-methoxy-1H-indol-3-yl)-methanone exhibits marked antiproliferative activity against KB and MKN45 cells with IC50 values of 8.8 and 10.5 nM, respectively, binds strongly to the colchicine binding site and leads to inhibition of tubulin polymerization. It also behaves as a vascular disrupting agent which suppresses the formation of capillaries. The C2-OH group in the A-ring of this compound not only retains the biological activity but has valuable physicochemical properties.
    日期: 2015-08
    關聯: Bioorganic and Medicinal Chemistry. 2015 Aug;23(15):4230-4236.
    Link to: http://dx.doi.org/10.1016/j.bmc.2015.06.043
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0968-0896&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000358440000012
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84937522856
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