C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/64 (2006.01) A61K 38/08 (2006.01)
Patent
CA 2563708
Compounds of Formula (I) are described in which the R1 group is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 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 le groupe R¿1? est tel que défini dans les spécifications et comprend la condensation de molécules de camptothecine en position 7 avec un cyclopeptide contenant la séquence RGD. Ces composés possèdent une forte affinité pour les récepteurs de l'intégrine ?¿v??¿3? et ?¿v??¿5? et avec une activité cytotoxique sélective sur des lignées de cellules tumorales humaines à des concentrations micromolaires.
Alloatti Domenico
Dal Pozzo Alma
Dallavalle Sabrina
Giannini Giuseppe
Merlini Lucio
Fetherstonhaugh & Co.
Istituto Nazionale Per Lo Studio E. La Cura Dei Tumori
Ni Minghong
Sigma-Tau Industrie Farmaceutiche Riunite S.p.a.
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