https://scholars.lib.ntu.edu.tw/handle/123456789/564783| Title: | Ring fusion strategy for the synthesis of anthra[2,3-d ]oxazole-2-thione-5,10-dione homologues as DNA topoisomerase inhibitors and as antitumor agents | Authors: | Chen C.-L. Liu F.-L. Lee C.-C. Chen T.-C. Chang W.-W. JIH-HWA GUH Ahmed Ali A.A. Chang D.-M. Huang H.-S. |
Keywords: | cell panel assay; mediated DNA relaxation NCI 60; Topoisomerase I | Issue Date: | 2014 | Journal Volume: | 87 | Start page/Pages: | 30-38 | Source: | European Journal of Medicinal Chemistry | Abstract: | The efficient synthesis of mono-substituted anthraquinones and ring fusion into anthra[2,3-d]oxazole-2-thione-5,10-dione derivatives were developed, and all the compounds were tested for their cytotoxicity against PC-3 cancer cell lines. Compounds 8, 14, 17 and 23 were selected by the NCI and 12, 17 and 19 were evaluated for topoisomerase I-mediated DNA relaxation. Among them, 17 appeared to be the most active compound of this series and not only showed higher inhibition when indicated from the low IC50values against PC-3 cancer cell line but also attenuated the in vitro topoisomerase I-mediated DNA relaxation at low micromolar concentrations. All test compounds exhibited different cytostatic and cytotoxic activities for further developing potential anticancer drugs. ? 2014 Elsevier Masson SAS. |
URI: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84907214737&doi=10.1016%2fj.ejmech.2014.09.016&partnerID=40&md5=ad9959f02db9fa7d620d28a5f646ac48 https://scholars.lib.ntu.edu.tw/handle/123456789/564783 |
ISSN: | 2235234 | DOI: | 10.1016/j.ejmech.2014.09.016 | SDG/Keyword: | 2 (3 chloropropionamido) 3 hydroxy anthraquinone; 2 (butylthio)anthra[2,3 d]oxazole 5,10 dione; 2 (chloroacetamido) 3 hydroxy anthraquinone; 2 (ethylthio)anthra[2,3 d]oxazole 5,10 dione; 2 (methylthio)anthra[2,3 d]oxazole 5,10 dione; 2 (propylthio)anthra[2,3 d]oxazole 5,10 dione; 2 [(2 fluorobenzyl)thio]anthra[2,3 d]oxazole 5,10 dione; 2 [(2 morpholinoethyl)thio]anthra[2,3 d]oxazole 5,10 dione; 2 [(4 fluorobenzyl)thio]anthra[2,3 d]oxazole 5,10 dione; 2 [2 (diethylamino)acetamido] 3 hydroxy anthraquinone; 2 [2 (n morpholin)acetamido] 3 hydroxy anthraquinone; 2 [2 (n piperidin)acetamido] 3 hydroxy anthraquinone; 2 [2 (pyrrolidinyl)acetamido] 3 hydroxy anthraquinone; 2 [3 (diethylamino)propionamido] 3 hydroxy anthraquinone; 2 [3 (n morpholin)propionamido] 3 hydroxy anthraquinone; 2 [3 (n piperidin)propionamido] 3 hydroxy anthraquinone; 2 [3 (n pyrrolidinyl)propionamido] 3 hydroxy anthraquinone; 2 [[2 (piperidin 1 yl)ethyl]thio]anthra[2,3 d]oxazole 5,10 dione; 2 [[3 (dimethylamino)propyl]thio]anthra[2,3 d]oxazole 5,10 dione; 2 [[3 (piperidin 1 yl)propyl]thio]anthra[2,3 d]oxazole 5,10 dione; anthraquinone derivative; anthra[2,3 b][1,4]oxazine 3,6,11 trione; anthra[2,3 d]oxazole 2 thione 5,10 dione; anthra[2,3 d]oxazole 2 thione 5,10 dione derivative; camptothecin; cytostatic agent; cytotoxic agent; DNA topoisomerase inhibitor; oxazole derivative; unclassified drug; unindexed drug; anthraquinone derivative; antineoplastic agent; DNA topoisomerase; DNA topoisomerase inhibitor; oxazole derivative; antineoplastic activity; antiproliferative activity; Article; cancer inhibition; concentration response; controlled study; cytostasis; drug cytotoxicity; drug potency; drug screening; drug synthesis; human; human cell; IC50; in vitro study; male; prostate cancer cell line; cell proliferation; chemical structure; chemistry; dose response; drug design; drug effects; pathology; Prostatic Neoplasms; structure activity relation; synthesis; tumor cell culture; Anthraquinones; Antineoplastic Agents; Cell Proliferation; DNA Topoisomerases, Type I; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Humans; Male; Molecular Structure; Oxazoles; Prostatic Neoplasms; Structure-Activity Relationship; Topoisomerase Inhibitors; Tumor Cells, Cultured [SDGs]SDG3 |
| Appears in Collections: | 藥學系 |
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