國家衛生研究院 NHRI:Item 3990099045/2842
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    题名: New analogues of AHMA as potential antitumor agents: Synthesis and biological activity
    作者: Chang, JY;Lin, CF;Pan, WY;Bacherikov, V;Chou, TC;Chen, CH;Dong, HJ;Cheng, SY;Tasi, TJ;Lin, YW;Chen, KT;Chen, LT;Su, TL
    贡献者: National Institute of Cancer Research
    摘要: A series of new analogues of 3-(9-acridinylamino)-5-hydroxymethylaniline (AHMA, 1) and AHMA-ethylcarbamate (2) were synthesized by introducing an O-alkylcarboxylic acid esters to the CH2OH function, displacing the CH2OH function with a dimethylaminocarboxamido group or with a methyl function introduced at the meta-, para- or ortho-position to the NH2 group to form 5-(9-acridinylamino)-m-toluidines (AMTs), 5-(9-acridinylamino)-p-toluidines (APTs) or 5-(9-acridinylamino)-o-toluidines (AOTs), respectively. The inhibitions of a variety of human tumor cell growth, interactions with DNA as well as inhibitory effect against topoisomerase 11 (Topo 11) of these new agents were studied. Among AMT, APT and AOT derivatives with dimethylaminoethylcarboxamido and Me at C4 and C5 of acridine moiety (i.e., 21c, 23c and 26c) were more cytotoxic than AHMA (1) and AHMA-ethylcarbamate (2), depending upon the tumor cell line tested. Detailed structure-activity relationships of the new analogues were studied. (C) 2003 Elsevier Ltd. All rights reserved.
    关键词: Biochemistry & Molecular Biology;Chemistry, Medicinal;Chemistry, Organic
    日期: 2003-11-17
    關聯: Bioorganic and Medicinal Chemistry. 2003 Nov;11(23):4959-4969.
    Link to: http://dx.doi.org/10.1016/j.bmc.2003.09.001
    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:000186614400012
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=0242266520
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