Chalcones having antiproliferative activity

Details Chalcones having antiproliferative activity Chalcones having antiproliferative activity

C - Chemistry, Metallurgy

07

D

C07D 213/50 (2006.01) A61K 31/12 (2006.01) A61K 31/40 (2006.01) A61K 31/44 (2006.01) C07C 45/74 (2006.01) C07C 49/84 (2006.01) C07C 225/22 (2006.01) C07C 233/33 (2006.01) C07D 209/12 (2006.01)

Patent

CA 2294278

Disclosed are compounds having general formula (A) wherein Ar représents phenyl, which may be unsubstituted or substituted by one, two or three substituents independently selected from Cl, Br, F, -OMe, NO2, CF3, C1-4 lower alkyl, -NMe2, -NEt2, -SCH3, -NHCOCH3; 2-thienyl; 2-furyl; 3-pyridyl; 4-pyridyl or 3-indolyl, and R represents -OCH2R1, in which R1 is selected from -CH-CMe2, -CMe-CH2, - C.ident.CH; with the proviso that where Ar represents phenyl, R is other than 3-methyl-2-butenyl. The compounds possess a valuable antiproliferation activity both on sensitive cancerous cells and on cells which are resistant to common chemotherapeutic drugs.

L'invention concerne des composés possédant la formule générale (A) dans laquelle Ar représente phényle, lequel peut n'être pas substitué ou l'être par un, deux ou trois substituants choisis indépendamment dans le groupe constitué par Cl, Br, F, -OMe, NO2, CF3, alkyle inférieur C1-4, -NMe2; -NEt2, -SCH3, -NHCOCH3; 2-thiényle; 2-furyle; 3-pyridyle; 4-pyridyle ou 3-indolyle, et R représente -OCH2R1, où R1 est choisi dans le groupe constitué par -CH=CMe2, -CMe=CH2, -CCH; à condition que lorsque Ar représente phényle, R soit différent de 3-méthyl-2-butényle. Ces composés possèdent une activité antiproliférante précieuse, à la fois sur des cellules cancéreuses sensibles et sur des cellules qui sont résistantes aux médicaments chimiothérapiques classiques.

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