Fluoroalkoxycombretastatin derivatives, methods for...

C - Chemistry – Metallurgy – 07 – C

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C07C 43/23 (2006.01) A61K 31/09 (2006.01) A61K 31/136 (2006.01) A61K 31/16 (2006.01) A61K 31/661 (2006.01) A61P 35/00 (2006.01) C07C 43/225 (2006.01) C07C 217/84 (2006.01) C07C 237/04 (2006.01) C07F 9/12 (2006.01)

Patent

CA 2660760

Combretastatin derivatives of formula (I) , preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms , R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.

La présente invention concerne des dérivés combrétastatine de formule (I), ainsi que leur préparation et leur utilisation. Dans la formule (I), Rf est un alkyle ayant de 1 à 8 atomes de carbone et de 1 à 17 atomes de fluor et R est une chaîne latérale amino, amino substituée, hydroxyle, nitro, halogéno, alkyloxy, phosphate ou acide aminé. Lesdits dérivés ont la capacité d'empêcher la polymérisation de microtubules et ils sont utiles pour le traitement des tumeurs et la néovascularisation.

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