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

Marcella Marcellini

Maria Ornella Tinti

Giuseppe Giannini

Mauro Marzi

Domenico Alloatti

Teresa Riccioni

The present invention is related to new derivatives of Combretastatin, of Formula obtained by total synthesis. The strategy developed for each of the compounds is to i) replace a halogen (i.e. fluorine atom) to hydrogen on olefinic bound; ii) replace an aromatic ring in a natural product with an amino-aromatic ring. Said compounds recognize and bind the tubulin site: are useful for treating pathological states which arise from or are exacerbated by cell proliferation&#x2014;as anticancer and/or antiangiogenic activity, in a mammal&#x2014;to pharmaceutical compositions comprising these compounds.

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Rome, Italy

Marcella Marcellini