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α-Halogenoacrylic Derivatives of Antitumor Agents

[ Vol. 9 , Issue. 1 ]


Romeo Romagnoli, Pier Giovanni Baraldi, Olga Cruz-Lopez, Carlota Lopez-Cara and Delia Preti   Pages 81 - 94 ( 14 )


In this review article we have reported a series of hybrid compounds characterized by the presence of a α- halogenocryloyl alkylating moiety of low chemical reactivity, linked to known antitumor agents or their active moieties. Among them, brostallicin (PNU-166196), was selected for clinical development and is now undergoing Phase II studies in patients with advanced or metastatic soft tissue sarcoma.


Antitumor agents, Distamycin A, apoptosis, α-bromoacryloyl, hybrid molecules


Dipartimento di Scienze Farmaceutiche, Universita di Ferrara, Via Fossato di Mortara 17-19, 44100- Ferrara, Italy.

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