Combretastatin analogs with tubulin binding activity

Details Combretastatin analogs with tubulin binding activity Combretastatin analogs with tubulin binding activity

C - Chemistry, Metallurgy

07

C

C07C 43/215 (2006.01) A61K 31/12 (2006.01) A61P 35/00 (2006.01) C07C 43/23 (2006.01) C07C 49/82 (2006.01)

Patent

CA 2611712

Analogs of combretastatin have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro- drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.

La présente invention concerne des analogues combrestatiniques faisant preuve d'une importante cytotoxicité ainsi que d'une remarquable aptitude à inhiber la polymérisation tubulinique. De tels composés sont d'excellents candidats cliniques pour le traitement de cancers humains. En outre, certains de ces ligands, en tant que pro-médicaments, sont vraisemblablement des chimiothérapiques tumeur-sélectifs à ciblage vasculaire ou présentant d'une activité de ciblage vasculaire permettant d'envisager une prévention sélective et/ou une destruction de vascularisations bénignes proliférantes.

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