MAX-PLANCK-GESELLSCHAFT ZUR FOERDERUNG DER WISSENSCHAFTEN E.V.
发明人:
DEL CAMPO BÈCARES, Aránzazu,GROPEANU, Radu Adrian,RITZ, Sandra,MAILAENDER, Volker
申请号：
EPEP2012/003098
公开号：
WO2013/029723A1
申请日:
2012.07.23
申请国别(地区):
WO
年份:
2013
代理人:
摘要：
The present invention provides novel photoactivatable paclitaxel derivatives wherein the C2 and C7 positions of the paclitaxel molecule are substituted with a photocleavable moiety such as a chromophore. Typically, the chromophore is selected from the group comprising 2-nitrobenzyl ethers, carbamates or carbonates and their 4,5-dialkoxy substituted variants 2-nitrophenylethyl ethers, carbamates or carbonates and their 4,5-dialkoxy substituted variants, or their p-substituted derivatives oc-carboxy-2-nitrobenzyl ethers, carbamates or carbonates and their 4,5-dialkoxy substituted variants 2(2-nitro- phenyl) ethyl ethers, carbamates or carbonates and their 4,5-dialkoxy substituted variants coumarin-4-ylmethyl ethers, or carbonates and their 7-alkoxy, 6, 7-dialkoxy, 6-bromo-7-alkoxy or 7-dialkylamino substituted variants p-hydroxyphenacyl ethers or carbamates and their meta-substituted derivatives or structurally related compounds. More specifically, the chromophore is 4, 5-dimethoxy-2- nitrobenyloxycarbonyl (Nvoc) or a structurally related compound. Further aspects of the invention relate to the use of these paclitaxel derivatives in biological, medical and pharmaceutical applications, in particular in cellbiology and cancer treatment. A closely related aspect is an antitumor medicament comprising the above paclitaxel derivatives.La présente invention concerne de nouveaux dérivés de paclitaxel photoactivables, dans lesquels les positions C2 et C7 de la molécule de paclitaxel sont substituées avec une fraction photoclivable telle quun chromophore. Le chromophore est généralement choisi dans le groupe comprenant les éthers, carbamates ou carbonates de 2-nitrobenzyle et leurs variantes à substitution 4,5-dialcoxy les éthers, carbamates ou carbonates de 2-nitrophényléthyle et leurs variantes à substitution 4,5-dialcoxy ou leurs dérivés à substitution p les éthers, carbamates ou carbonates doc-carboxy-2-nitrobenzyle et leurs variantes à substitution 4,5-dialcoxy les éthe
