Synthesis and biological activity of dialkylphosphocholines.
A series of dialkylphosphocholines were prepared and evaluated for their biological activity. The antiprotozoal activity was determined against Acanthamoeba lugdunensis. Compound 15 exhibited excellent trophocidal activity. None of the tested dialkylphosphocholines exhibited better fungicidal activity against Candida albicans than miltefosine. The antineoplastic activity was determined against HeLa. The most cytotoxic was compound 10, which was more active against tumor cells as against normal cells.
Lukác
Milos
M
Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University, Kalinciakova 8, 83232 Bratislava, Slovakia. lukac@fpharm.uniba.sk
Mrva
Martin
M
Fischer-Fodor
Eva
E
Lacko
Ivan
I
Bukovský
Marián
M
Miklásová
Natalia
N
Ondriska
Frantisek
F
Devínsky
Ferdinand
F
D000048:Acanthamoeba; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology*; D000981:Antiprotozoal Agents; D002176:Candida albicans / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010767:Phosphorylcholine / Q000031:analogs & derivatives; D010936:Plant Extracts; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D000981:Antiprotozoal Agents; D010936:Plant Extracts; D010767:Phosphorylcholine; C039128:miltefosine