Synthesis of new Targretin analogues that induce apoptosis in leukemia HL-60 cells.
Four new analogues of Targretin where the carboxylic acid function was replaced by an N,N-dimethyl-S-aryl carbamate or N,N-dimethyl-O-arylthiocarbamate function, were synthesized. Compounds 5, 6 and 7 have shown to be more potent than the parent compound to induce apoptosis of HL-60 cells.
Winum
Jean-Yves
JY
Laboratoire de Chimie Biomoléculaire, UMR 5032, Université Montpellier II - CNRS - Laboratoires Mayoly Spindler, ENSCM, 8 Rue de l'Ecole Normale, 34296 Montpellier Cedex, France.
Baghdiguian
Stephen
S
Commes
Thérèse
T
Leydet
Alain
A
Montero
Jean-Louis
JL
D016588:Anticarcinogenic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D000077610:Bexarotene; D002219:Carbamates / Q000138:chemical synthesis / Q000494:pharmacology; D018922:HL-60 Cells; D006801:Humans; D007938:Leukemia / Q000473:pathology*; D018168:Receptors, Retinoic Acid / Q000819:agonists; D047488:Retinoid X Receptors; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D014157:Transcription Factors / Q000819:agonists
D016588:Anticarcinogenic Agents; D002219:Carbamates; D018168:Receptors, Retinoic Acid; D047488:Retinoid X Receptors; D013764:Tetrahydronaphthalenes; D014157:Transcription Factors; D000077610:Bexarotene