C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 69/017 (2006.01) A61K 31/223 (2006.01) A61K 31/225 (2006.01) A61K 31/661 (2006.01) A61K 31/704 (2006.01) A61P 35/00 (2006.01) C07C 69/00 (2006.01) C07C 229/08 (2006.01) C07C 229/36 (2006.01) C07D 209/20 (2006.01) C07F 9/09 (2006.01) C07H 15/244 (2006.01)
Patent
CA 2446429
The invention relates to aloe-emodin (AE) derivatives and their use as anticancer drugs. Said derivatives show a specific cytotoxicity to tumour cells, also of neuroectodermal origin, to which they may in particular act as aloe- emodin prodrugs. Said pharmacological profile makes them particularly suitable for use in the treatment of neoplasias. Therefore, pharmaceutical compositions containing said compound may be usefully used in the treatment of neoplasias. It has surprisingly been found that aloe-emodin derivatives in position 3' (bearing either a positive or negative charge) exhibit improved solubility properties and, at the same time, in vitro show cytotoxicity to tumour cells, also of neuroectodermal origin.
L'invention concerne des dérivés d'aloe-émodine (AE) et leur utilisation comme médicaments contre des cancers. Ces dérivés présentent une cytotoxicité spécifique aux cellules tumorales, également d'origine neuroectodermique, sur lesquelles ils peuvent en particulier agir comme promédicaments aloe-émodine. Ce profil pharmacologique les rend notamment appropriés au traitement de la néoplasie. Des compositions pharmaceutiques contenant ces composés peuvent donc servir dans le traitement de la néoplasie. Selon la présente invention, les dérivés d'aloe-émodine en position 3' (porteurs d'une charge positive ou négative) possèdent des propriétés de solubilité améliorées, et présentent, à la fois, in vitro une cytotoxicité vis-à-vis des cellules tumorales, également d'origine neuroectodermique.
Carli Modesto
Palu' Giorgio
Pecere Teresa
Zagotto Giuseppe
Marks & Clerk
Universita Degli Studi Di Padova
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