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Please use this identifier to cite or link to this item:
http://ir.nhri.org.tw/handle/3990099045/2842
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Title: | New analogues of AHMA as potential antitumor agents: Synthesis and biological activity |
Authors: | 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 |
Contributors: | National Institute of Cancer Research |
Abstract: | 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. |
Keywords: | Biochemistry & Molecular Biology;Chemistry, Medicinal;Chemistry, Organic |
Date: | 2003-11-17 |
Relation: | 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 |
Appears in Collections: | [陳立宗] 期刊論文 [張俊彥] 期刊論文
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