期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 24, 页码 6914-6917出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.10.081
关键词
Anti-tumoral; Breast cancer; Imidazolidin-4-ones; Malaria; Primaquine; Quinolines
资金
- Portuguese Foundation for Science and Technology (FCT) [PTDC/QUI/65142/2006, PTDC/QUI/65501/2006, CONC-REEQ/275/QUI, REDE/1517/RMN/2005, SFRH/BPD/48345/2008, SFRH/BD/38883/2007]
- Fundação para a Ciência e a Tecnologia [SFRH/BD/38883/2007] Funding Source: FCT
The growth inhibitory activity of imidazoquines, antimalarial imidazolidin-4-ones derived from primaquine, on human cancer cell lines HT-29, Caco-2, and MCF-7 has been evaluated. Primaquine, N-dipeptidyl-primaquine derivatives, and other quinolines have been included in the study for comparison purposes. Primaquine and some of its derivatives were significantly active against the MCF-7 human breast cancer cell line, so these compounds might represent useful leads targeted at the development of novel specific agents against breast cancer. Conversely, all compounds were generally inactive against HT-29, with only one of the imidazoquines having IC50 below 50 mu M. Activities against the Caco-2 cell line were modest and did not follow any defined trend. (C) 2009 Elsevier Ltd. All rights reserved.
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