Synthesis of Bioconjugate Sesterterpenoids with Phospholipids and Polyunsaturated Fatty AcidsReport as inadecuate




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Departamento de Química Orgánica, Universidad de Salamanca, Plaza de los Caídos 1-5, 37008 Salamanca, Spain

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Instituto de Biología Molecular y Celular del Cáncer, Centro de Investigación del Cáncer, CSIC-Universidad de Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain

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Laboratory of Cell Death and Cancer Therapy, Department of Cellular and Molecular Medicine, Centro de Investigaciones Biológicas, CSIC, C-Ramiro de Maeztu 9, 28040 Madrid, Spain





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Academic Editors: Jean Jacques Vanden Eynde and Annie Mayence

Abstract A series of sesterterpenoid bioconjugates with phospholipids and polyunsaturated fatty acids PUFAs have been synthesized for biological activity testing as antiproliferative agents in several cancer cell lines. Different substitution analogues of the original lipidic ether edelfosine 1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphocholine are obtained varying the sesterterpenoid in position 1 or 2 of the glycerol or a phosphocholine or PUFA unit in position 3. Simple bioconjugates of sesterterpenoids and eicosapentaenoic acid EPA have been obtained too. All synthetic derivatives were tested against the human tumour cell lines HeLa cervix and MCF-7 breast. Some compounds showed good IC50 0.3 and 0.2 μM values against these cell lines. View Full-Text

Keywords: antitumoural; bioconjugates; ether lipidics; edelfosine; sesterterpenolides; PUFAs antitumoural; bioconjugates; ether lipidics; edelfosine; sesterterpenolides; PUFAs





Author: Ana Gil-Mesón 1, Alejandro M. Roncero 1, Ignacio E. Tobal 1, Pilar Basabe 1, David Díez 1, Faustino Mollinedo 2,3 and Isidro S. Marcos 1,*

Source: http://mdpi.com/



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