Conjugates of integrin receptor antagonists and a cytostatic agent having specifically cleavable linking units

摘要

The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to alpha v beta 3 integrin antagonists via preferred linking units which can be selectively cleaved by enzymes such as metallo matrixproteases (MMPs), i.e. by enzymes which can especially be found in tumor tissue. The preferred linking units guarantee the serum stability of the conjugate of cytostatic and alpha v beta 3 integrin antagonist and, at the same time, the desired intracellular action within tumour cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic. <CHEM> <CHEM> <CHEM>