Overcoming doxorubicin-resistance in the NCI/ADR-RES model cancer cell line by novel anthracene-9,10-dione derivatives

  • Bioorg Med Chem Lett. 2013 Nov 15;23(22):6156-60. doi: 10.1016/j.bmcl.2013.09.004.
Supranee Sangthong  1 ,  Helen Ha ,  Thapong Teerawattananon ,  Nattaya Ngamrojanavanich ,  Nouri Neamati ,  Nongnuj Muangsin
Affiliations
  • 1. Program of Biotechnology, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
PMID: 24095089 DOI: 10.1016/j.bmcl.2013.09.004
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.

Keywords
Anthraquinone derivatives; Cytotoxic mechanism; Doxorubicin-resistance.