國家衛生研究院 NHRI:Item 3990099045/2723
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    题名: Synthesis and antitumor activity of 5-(9-acridinylamino)anisidine derivatives
    作者: Bacherikov, VA;Chang, JY;Lin, YW;Chen, CH;Pan, WY;Dong, H;Lee, RZ;Chou, TC;Su, TL
    贡献者: National Institute of Cancer Research
    摘要: A series of 5-(9-acridinylamino)anisidines were synthesized by condensing methoxy-substituted 1,3-phenylenediamines (10 and 11) with 9-chloroacridine derivatives to form 5-(9-acridinylamino)-m-anisidines (AMAs, 14a-e) and 5-(9-acridinylamino)-o-anisidines (AOAs, 15a-e). 5-(9-Acridinylamino)-p-anisidines (APAs, 17a-e) were synthesized by reacting 2-methoxy-5-nitroaniline (12) with 9-anilinoacridines, followed by reduction. The cytotoxic inhibition of growth of various human tumor cells in culture, inhibitory effects against topoisomerase II, and DNA interaction of these agents were studied. The structure-activity relationship studies revealed the following degree of potency: AOAs > AMAs > APAs. They also revealed that the newly synthesized derivatives bearing CONH2NH2NMe2 and Me substituents at C4 and C5 positions of the acridine chromophore (i.e., AMA 14e, AOA 15e, and APA 17e) exhibited significant cytotoxicity against human tumor cell growth in vitro. AOA (15e) was the most potent among these derivatives, which resulted in 60% suppression of tumor volume at a dose of 20 mg/kg (Q2D x 9), intravenous injection on day 26 in nude mice bearing human breast carcinoma MX-1 xenografts. (c) 2005 Elsevier Ltd. All rights reserved.
    关键词: Biochemistry & Molecular Biology;Chemistry, Medicinal;Chemistry, Organic
    日期: 2005-12-01
    關聯: Bioorganic and Medicinal Chemistry. 2005 Dec;13(23):6513-6520.
    Link to: http://dx.doi.org/10.1016/j.bmc.2005.07.018
    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:000232959200023
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=27544472329
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