Overcoming doxorubicin-resistance in the NCI/ADR-RES model cancer cell line by novel anthracene-9,10-dione derivatives |
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| Authors: | Supranee Sangthong Helen Ha Thapong Teerawattananon Nattaya Ngamrojanavanich Nouri Neamati Nongnuj Muangsin |
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| Institution: | 1. Program of Biotechnology, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand;2. Department of Pharmacology and Pharmaceutical Science, School of Pharmacy, University of Southern California, 1985 Zonal Avenue, Los Angeles, CA 90033, USA;3. Department of Chemistry, Faculty of Science, Chulalongkorn University, 254 Phayathai Rd., Phatumwan, Bangkok 10330, Thailand |
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| Abstract: | Overcoming drug resistance with remarkable cytotoxic activity by anthracene-9,10-dione derivatives would offer a potential therapeutic strategy. In this study, we report the synthesis and the cytotoxicity of a novel set of anthraquninones. (4-(4-Aminobenzylamino)-9,10-dioxo-9,10-dihydroanthracen-1-yl-4-methylbenzenesulfonate) (3) has excellent in vitro cytotoxicity against doxorubicin-resistant cancer cell line (IC50 = 0.8 μM), 20-fold higher than doxorubicin. The cytotoxic effect via G2/M arrest does not appear to be ROS. |
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| Keywords: | Doxorubicin-resistance Cytotoxic mechanism Anthraquinone derivatives |
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