國家衛生研究院 NHRI:Item 3990099045/3334
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    題名: Structure-activity relationship studies of 3-aroylindoles as potent antimitotic agents
    作者: Liou, JP;Mahindroo, N;Chang, CW;Guo, FM;Lee, SWH;Tan, UK;Yeh, TK;Kuo, CC;Chang, YW;Lu, PH;Tung, YS;Lin, KT;Chang, JY;Hsieh, HP
    貢獻者: Division of Biotechnology and Pharmaceutical Research;National Institute of Cancer Research
    摘要: The concise synthesis and structure-activity relationship (SAR) studies of 3-aroylindoles were carried out in an effort to improve the potency and solubility of anticancer drug candidate BPR0L075 (8) by exploring structure modifications through three regimens: substitution of the B ring, at the N1 position, and of the 3-carbonyl linker. The SAR information revealed that the methoxy group of the B ring could be replaced with an electron-donating group such as methyl (in compound 9) or N,N-dimethylamino (in compound 13) while retaining both strong cytotoxic and antitubulin activities. The introduction of amide (compounds 30-33) and carbamate (compounds 34-37) functionalities at the N1 position of 8 gave analogues with potent antiproliferative activities. The cytotoxic potency of 8 was improved by replacing the carbonyl group with sulfide (compound 41) or oxygen (compound 43), indicating that the carbonyl moiety is important but not essential. The N,N-dimethylamino derivative 13 not only displayed potent cytotoxicity and antitubulin activity, but also showed a markedly improved physicochemical profile relative to the parent compound.
    日期: 2006-10
    關聯: ChemMedChem. 2006 Oct;1(10):1106-1118.
    Link to: http://dx.doi.org/10.1002/cmdc.200600125
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1860-7179&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000202946300010
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=33750339847
    顯示於類別:[謝興邦] 期刊論文
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    [郭靜娟] 期刊論文
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