Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 102, Issue -, Pages 303-309Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.08.006
Keywords
Anthraquinone; Nitrogen mustard; Synthesis; Antitumor activity
Categories
Funding
- Major Program of Natural Science Foundation of Jiangsu Higher Education Institutions [12KJA150005]
- NIGMS [1U54GM104940]
- Natural Science Foundation of Jiangsu Province [BK2012576]
- NIMHD [2G12MD007595]
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A series of hydroxyanthraguinones having an alkylating N-mustard pharmacophore at 1'-position were synthesized via a bioisostere approach to evaluate their cytotoxicity against four tumor cell lines (MDA-MB-231, HeLa, MCF-7 and A549). These compounds displayed significant in vitro cytotoxicity against MDA-MB-231 and MCF-7 cells, reflecting the excellent selectivity for the human breast cancer. Among them, compound 5k was the most cytotoxic with IC50 value of 0.263 nM and is more potent than DXR (IC50 = 0.294 mu M) in inhibiting the growth of MCF-7 cells. The excellent cytotoxicity and good selectivity of compound 5k suggest that it could be a promising lead for further design and development of anticancer agents, especially for breast cancer. (C) 2015 Elsevier Masson SAS. All rights reserved.
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