Synthesis and photocytotoxic activity of new alpha-methylene-gamma-butyrolactone-psoralen heterodimers.
The synthesis of a new alpha-methylene-gamma-butyrolactone-psoralen heterodimer 2 is reported. Its photoantiproliferative activity and skin phototoxicity were compared with that of 5-methoxypsoralen (5-MOP) and another heterodimer 1. Both derivatives show a significant phototoxicity toward malignant cell lines including melanoma cells A375 compared to their intrinsic cytotoxicity in the dark. Both compounds were found to be nonphototoxic on mice skin and therefore could be active potential drugs in photochemotherapy.
Ropp
Sandrine
S
Laboratoire de Dermatochimie, UMR 7123, Université Louis Pasteur, Clinique Dermatologique, CHU, F-67091 Strasbourg Cedex, France.
Guy
Julia
J
Berl
Valérie
V
Bischoff
Pierre
P
Lepoittevin
Jean-Pierre
JP
D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects / Q000528:radiation effects; D019281:Dimerization; D005260:Female; D005363:Ficusin / Q000009:adverse effects / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011564:Furocoumarins; D006801:Humans; D020128:Inhibitory Concentration 50; D007783:Lactones / Q000009:adverse effects / Q000138:chemical synthesis* / Q000494:pharmacology*; D008545:Melanoma / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D008807:Mice, Inbred BALB C; D015394:Molecular Structure; D010778:Photochemotherapy; D012867:Skin / Q000187:drug effects / Q000473:pathology
D000970:Antineoplastic Agents; D011564:Furocoumarins; D007783:Lactones; C494927:alpha-methylene-gamma-butyrolactone-psoralen; D005363:Ficusin