Tubulin binding ligands and corresponding prodrug constructs

Details Tubulin binding ligands and corresponding prodrug constructs Tubulin binding ligands and corresponding prodrug constructs

C - Chemistry, Metallurgy

07

F

C07F 9/6553 (2006.01) A61K 31/075 (2006.01) A61K 31/12 (2006.01) A61K 31/13 (2006.01) A61K 31/343 (2006.01) A61K 31/381 (2006.01) A61K 31/66 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 27/02 (2006.01) A61P 35/00 (2006.01) C07C 43/215 (2006.01) C07C 43/23 (2006.01) C07C 45/51 (2006.01) C07C 45/64 (2006.01) C07C 49/84 (2006.01) C07C 205/45 (2006.01) C07C 217/84 (2006.01) C07C 217/94 (2006.01) C07C 225/22 (2006.01) C07D 307/80 (2006.01) C07D 307/81 (2006.01) C07D 333/56 (2006.01) C07D 333/58 (2006

Patent

CA 2407967

A diverse set of tubulin binding ligands have been discovered which are structural by characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, and phosphoramides capable of demonstrating selective targeting and destruction of tumor cell vasculature.

On a découvert un groupe hétérogène de ligands de liaison de tubuline qui, du point de vue structurel se caractérisent globalement par une ossature moléculaire semi-rigide qui est capable de maintenir des distances d'empilement aryle-aryle, pseudo pi, appropriées à la reconnaissance de la tubuline par les molécules. Sous une forme phénolique ou amino, ces ligands peuvent être ensuite fonctionnalisés pour préparer des esters phosphoriques, des sels de phosphate et des phosphoramides capables d'effectuer un ciblage sélectif et de détruire le réseau des cellules tumorales.

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