國家衛生研究院 NHRI:Item 3990099045/6223
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    题名: 5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. Part 2. The impact of bridging groups at position C-2
    作者: Lee, HY;Chang, JY;Nien, CY;Kuo, CC;Shih, KH;Wu, CH;Chang, CY;Lai, WY;Liou, JP
    贡献者: National Institute of Cancer Research
    摘要: A variety of studies on the modification of combretastatin A-4 triggered our interest in the impact of the linkers between the 3,4,5-trimethoxyphenyl ring and 5-amino-6-methoxyquinoline on biological activity. The replacement of the carbonyl group with bond, amine, ether, sulfide, and sulfone groups was evaluated in this study. The results showed that compounds 14 and 15 containing sulfide and sulfone groups between the 3,4,5-trimethoxyphenyl ring (A-ring) and 5-amino-6-methoxyquinoline exhibited substantial antiproliferative activity against KB, HT29, and MKN45 cells with mean IC50 values of 42 and 12 nM, respectively. 15 inhibited the tubulin polymerization with an IC 50 value of 2.0 μM, similar to that with CA4. The continued work on the C-5 substituents of 3′,4′,5′-trimethoxybenzoyl-6- methoxyquinoline derivatives demonstrated that compound 7 possessing OH at C-5 exhibited excellent antiproliferative activity with mean IC50 values of 3.4 nM and microtubule destabilizing potency with an IC50 of 1.5 μM, comparable to that of CA4 (IC50 = 1.9 μM). It also exhibited substantial vascular disrupting effects. Compounds 7 and 15 exhibited significant efficacy against MDR/MRP-related drug-resistant cell lines (KB-vin10, KB-S15, and KB-7D) with mean IC50 values of 6.7 and 2.6 nM, respectively.
    日期: 2011-12-22
    關聯: Journal of Medicinal Chemistry. 2011 Dec 22;54(24):8517-8525.
    Link to: http://dx.doi.org/10.1021/jm201031f
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000297946300025
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84055176276
    显示于类别:[郭靜娟] 期刊論文
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