期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 102, 期 -, 页码 661-676出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.07.052
关键词
Thiadiazoles; Anthra[1,2-c][1,2,5]thiadiazole-6,11-dione; SRB assay; NCI 60-cell panel assay; Apoptosis
资金
- National Cancer Institute, National Institutes of Health (NIH-NCI)
- Ministry of Science and Technology
- Taipei Medical University [NSC101-2113-M-016, MOST103-2113-M-038-002, TMU102-AE1-B32, TMUTOP-103003-1, NSC102-2314-B-016-048-MY2]
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. (C) 2015 Elsevier Masson SAS. All rights reserved.
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