255386-95-9Relevant academic research and scientific papers
Novel photoactivatable paclitaxel derivatives and uses thereof, in particular in cellbiology and cancer treatment
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Paragraph 0016-0017; 0044-0047, (2013/03/26)
The present invention provides novel photoactivatable paclitaxel derivatives wherein at least the C7 position, preferably both the C2' and C7 positions, of the paclitaxel molecule is/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; α-carboxy-2-nitrobenzyl ethers, carbamates or carbonates and their 4,5-dialkoxy substituted variants; 2(2-nitrophenyl)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.
NOVEL PHOTOACTIVATABLE PACLITAXEL DERIVATIVES AND USES THEREOF, IN PARTICULAR IN CELLBIOLOGY AND CANCER TREATMENT
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Page/Page column 13; 14, (2013/03/28)
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.
