Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 93, Issue -, Pages 263-273Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.02.014
Keywords
Acanthamoeba; Alkylphosphocholines; Candida albicans; Cytotoxic activity; Cut-off effect; SAR
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Funding
- Slovak Research and Development Agency [APVV-0516-12]
- Research and Development Operational Programme - ERDF [ITMS 26240120034, ITMS 26240220086]
- Romanian UEFISCDI Grant for Exploratory Research Projects [PN-II-ID-PCE-2011-3-1057, 250/2011]
- [UK/123/2014]
- [UK/263/2014]
- [VEGA 1/0796/12]
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Twelve derivatives of hexadecylphosphocholine (miltefosine) were synthesized to determine how the position and length of the alkyl chain within the molecule influence their biological activities. The prepared alkylphosphocholines have the same molecular formula as miltefosine. Activity of the compounds was studied against a spectrum of tumour cells, two species of protozoans, bacteria and yeast. Antitumour efficacy of some alkylphosphocholines measured up on MCF-7, A2780, HUT-78 and THP-1 cell lines was higher than that of miltefosine. The compounds showed antiprotozoal activity against Acanthamoeba lugdunensis and Acanthamoeba quina. Some of them also possess fungicidal activity against Candida albicans equal to miltefosine. No antibacterial activity was observed against Staphylococcus aureus and Escherichia coil. A difference in position of a long hydrocarbon chain within the structure with maximum efficacy was observed for antitumour, antiprotozoal and antifungal activity. (C) 2015 Elsevier Masson SAS. All rights reserved.
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