Synthesis of Bioconjugate Sesterterpenoids with Phospholipids and Polyunsaturated Fatty Acids.
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.
['Gil-Mesón|Ana|A|', 'Roncero|Alejandro M|AM|', 'Tobal|Ignacio E|IE|', 'Basabe|Pilar|P|', 'Díez|David|D|', 'Mollinedo|Faustino|F|', 'Marcos|Isidro S|IS|']
D000970:Antineoplastic Agents D049109:Cell Proliferation D005231:Fatty Acids, Unsaturated D005260:Female D006367:HeLa Cells D006801:Humans D061986:MCF-7 Cells D010742:Phospholipid Ethers D010743:Phospholipids D054830:Sesterterpenes
bioconjugates PUFAs edelfosine antitumoural ether lipidics sesterterpenolides