Camptothecin derivatives conjugated in position 20 with...

Details Camptothecin derivatives conjugated in position 20 with... Camptothecin derivatives conjugated in position 20 with...

A - Human Necessities

61

K

A61K 47/48 (2006.01) A61P 31/12 (2006.01) A61P 33/00 (2006.01) A61P 35/00 (2006.01) A61P 35/04 (2006.01)

Patent

CA 2562572

Compounds or formula (I) are described, in which R and R1 groups are as defined here below and include the condensation of the camptothecin molecule in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors .alpha.v.beta.3 and .alpha.v.beta.5 and with selective cytotoxic activity on human tumor cell lines at micromolar concentrations.

La présente invention concerne des composés représentés par la formule (I), dans laquelle, les groupes R et R¿1? sont tels que définis ci-dessous et comprennent la condensation de la molécule de camptothécine à la position 20 avec un cyclopeptide contenant la séquence RGD. Ces composés présentent à la fois une affinité élevée pour les récepteurs intégrines ?¿v??¿3? et ?¿v??¿5? et une activité cytotoxique sélective sur des lignées cellulaires tumorales humaines à des concentrations micromolaires.

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