https://scholars.lib.ntu.edu.tw/handle/123456789/454784
標題: | Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives | 作者: | Lee C.-C. Huang K.-F. Lin P.-Y. Huang F.-C. Chen C.-L. Chen T.-C. JIH-HWA GUH JING-JER LIN Huang H.-S. |
公開日期: | 2012 | 卷: | 47 | 期: | 1 | 起(迄)頁: | 323-336 | 來源出版物: | European Journal of Medicinal Chemistry | 摘要: | A series of diversely asymmetrical mono- or disubstituted 1,2-diamidoanthraquinone derivatives were synthesized and evaluated for drug-induced cytotoxicity by SRB assay, telomerase inhibitory activity by TRAP assay, and hTERT expression by SEAP assay. Interestingly, compounds 4, 11, 21, 32 and 36 exhibited selective potent antiproliferative activities by NCI with IC 50 values in the micromolar range. Of these, only compound 8 showed an IC 50 value of 0.95 μM against PC-3 cell lines (human prostate cancer) by SRB assay. All the synthesized compounds exhibited a poor or modest telomerase inhibitory activity by TRAP assay suggesting another mode of action for these compounds. Compound 11 showed broad inhibition against different types of cancer cell lines in the micromolar and submicromolar range. ? 2011 Elsevier Masson SAS. All rights reserved. |
URI: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84855780132&doi=10.1016%2fj.ejmech.2011.10.059&partnerID=40&md5=3938787fc1ec411d19b55987974c8066 https://scholars.lib.ntu.edu.tw/handle/123456789/454784 |
ISSN: | 0223-5234 | DOI: | 10.1016/j.ejmech.2011.10.059 | SDG/關鍵字: | 1 (2 chlorobenzamido) 2 (chloroacetamido) anthraquinone; 1 (2 fluorobenzamido) 2 (chloroacetamido) anthraquinone; 1 (2 methylbenzamido) 2 (chloroacetamido) anthraquinone; 1 (3 fluorobenzamido) 2 (chloroacetamido) anthraquinone; 1 (3 methylbenzamido) 2 (chloroacetamido) anthraquinone; 1 (4 chlorobenzamido) 2 (chloroacetamido) anthraquinone; 1 (4 fluorobenzamido) 2 (chloroacetamido) anthraquinone; 1 (amino) 2 (chloroacetamido) anthraquinone; 1 (benzamido) 2 (chloroacetamido) anthraquinone; 1 [(2 furoyl)amido] 2 (chloroacetamido) anthraquinone; 1 [(2,5 dimethyl 3 furoyl)amido] 2 (chloroacetamido) anthraquinone; 1 [(3 chloropropanyl)amido] 2 (chloroacetamido) anthraquinone; 1 [(4 chlorobutanyl)amido] 2 (chloroacetamido) anthraquinone; 1 [(5 isoxazolecarbonyl)amido] 2 (chloroacetamido) anthraquinone; 1 [2 (4 fluorophenyl)acetylamido] 2 (chloroacetamido) anthraquinone; 1 [2 (phenoxy)acetylamido] 2 (chloroacetamido) anthraquinone; 1 [2 (phenyl)acetylamido] 2 (chloroacetamido) anthraquinone; 1 [2 (phenylsulfanyl)acetylamido] 2 (chloroacetamido) anthraquinone; 1 [2 (trifluoromethyl)benzamido] 2 (chloroacetamido) anthraquinone; 1 [3 (trifluoromethyl)benzamido] 2 (chloroacetamido) anthraquinone; 1 [4 (trifluoromethyl)benzamido] 2 (chloroacetamido) anthraquinone; 1, 2 bis (chloroacetamido) anthraquinone; 1,2 bis (3 chloropropionamido) anthraquinone; 1,2 bis (4 chlorobutyramido) anthraquinone; 1,2 bis (4 methylbenzamido) anthraquinone; anthraquinone derivative; telomerase; telomerase reverse transcriptase; unclassified drug; unindexed drug; antineoplastic activity; article; cancer cell culture; controlled study; drug determination; drug inhibition; drug mechanism; drug potency; drug structure; drug synthesis; human; human cell; human cell culture; IC 50; prostate cancer; Anthraquinones; Cell Line, Tumor; Cell Proliferation; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Humans; Inhibitory Concentration 50; Telomerase |
顯示於: | 生物化學暨分子生物學科研究所 |
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