Fluorescent phenylpolyene analogues of the ether phospholipid edelfosine for the selective labeling of cancer cells.
Edelfosine (ET-18-OCH3), a synthetic antitumor ether lipid, is taken up by malignant but not by normal cells, triggering apoptosis in a large variety of human tumor cells. The synthesis of the first fluorescent edelfosine analogue (6), with apoptotic activity comparable to that of the parent drug, is described. Fluorescence microscopy experiments show that 6 selectively labels human cancer cells, accumulating into specific domains of the plasma membrane.
Instituto de Química Orgánica, C.S.I.C., Juan de la Cierva 3, E-28006 Madrid, Spain.
Ernesto
E
Quesada
Javier
J
Delgado
Consuelo
C
Gajate
Faustino
F
Mollinedo
A Ulises
AU
Acuña
Francisco
F
Amat-Guerri
D017209:Apoptosis; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D019169:Jurkat Cells; D008214:Lymphocytes / Q000473:pathology; D008856:Microscopy, Fluorescence; D010742:Phospholipid Ethers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D005456:Fluorescent Dyes; D010742:Phospholipid Ethers; C026659:edelfosine