https://scholars.lib.ntu.edu.tw/handle/123456789/564774| Title: | Ring fusion strategy for synthesis and lead optimization of sulfur-substituted anthra[1,2-c[[1,2,5]thiadiazole-6,11-dione derivatives as promising scaffold of antitumor agents | Authors: | Lee Y.-R. Chen T.-C. Lee C.-C. Chen C.-L. Ahmed Ali A.A. Tikhomirov A. JIH-HWA GUH Yu D.-S. Huang H.-S. |
Keywords: | Anthra[1 2-c][1 2 5]thiadiazole-6 11-dione; Apoptosis; NCI 60-cell panel assay; SRB assay; Thiadiazoles | Issue Date: | 2015 | Journal Volume: | 102 | Start page/Pages: | 661-676 | Source: | European Journal of Medicinal Chemistry | Abstract: | A series of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-diones were synthesized and evaluated using the cell proliferations, apoptosis and NCI-60 cell panel assays. Also, the signaling pathways that account for their activities were investigated. Compounds 2, 3, 4a, 4d, 4f, 4i, 4k, 5b, 5c, 5d, 5f, 5g, 6b, 6c, 6d, 6e, 6g, 7a and 7g were selected by NCI. Among the tested compounds, 6g appeared to be the most active compound of this series that not only induced apoptosis in DU-145 cancer cells but also attenuated the ERK1/2 and p38 signaling pathways. All test compounds exhibited diverse cytostatic and cytotoxic activities that warrant further development as potential anticancer agents. ? 2015 Elsevier Masson SAS. |
URI: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84941197893&doi=10.1016%2fj.ejmech.2015.07.052&partnerID=40&md5=f3b21eca188be28a62ee4ddab264f7d9 https://scholars.lib.ntu.edu.tw/handle/123456789/564774 |
ISSN: | 2235234 | DOI: | 10.1016/j.ejmech.2015.07.052 | SDG/Keyword: | 4 (2 bromophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (2 chlorophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (2 ethylphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (2 fluorophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (2 isopropylphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (2,4 difluorophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (2,4 dimethylphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (2,5 dichlorophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (2,6 dimethylphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (3 bromophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (3 chlorophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (3 ethoxyphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (3 fluorophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (3 methoxyphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (3,5 dimethylphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (4 bromophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (4 chlorophenylthio)anthra[1,2-c][1,2,5]thiadiazole-6,11- dione; 4 (4 ethylphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (4 fluorophenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (4 isopropylphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (4 methoxyphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (4 tert butylphenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (benzylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (isopropylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (o tolylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 (phenylthio)anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; 4 [4 (methylthio)phenylthio]anthra[1,2 c][1,2,5]thiadiazole 6,11 dione; antineoplastic agent; sulfur substituted anthra[1,2 c ][1,2,5]thiadiazole 6,11 dione derivative; unclassified drug; unindexed drug; 4-(isopropylthio)anthra(1,2-c)(1,2,5)thiadiazole-6,11-dione; anthraquinone derivative; antineoplastic agent; sulfur; thiadiazole derivative; antineoplastic activity; apoptosis; Article; assay; cancer cell; cell proliferation; controlled study; cytotoxicity; drug synthesis; human; human cell; national health organization; chemical structure; chemistry; drug effects; drug screening; structure activity relation; synthesis; tumor cell line; Anthraquinones; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Drug Screening Assays, Antitumor; Humans; Molecular Structure; Structure-Activity Relationship; Sulfur; Thiadiazoles [SDGs]SDG3 |
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