Sigma-tau Industrie Farmaceutiche Riunite S.p.a.

Instituto Nazionale Per Lo Studio E La Cura Dei Tumori

Alma Dal Pozzo

Maria Ornella Tinti

Sergio Penco

Claudio Pisano

Giuseppe Giannini

Loredana Vesci

Franco Zunino

Lucio Merlini

Sabrina Dallavalle

Domenico Alloatti

Ni Minghong

Ni Ming Hong

Ni Ming Hong Hong

Compounds of Formula (I) are described in which the Rgroup 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 &#x3b1;&#x3b2;and &#x3b1;&#x3b2;and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.

Camptothecins conjugated in position 7 to cyclic peptides as cytostatic agents

Compounds of Formula (I) are described: in which the Rgroup is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors &#x3b1;&#x3b2;and &#x3b1;&#x3b2;and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.

7-t-butoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists

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Rome, Italy

Alma Dal Pozzo