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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

α-Halogenoacrylic Derivatives of Antitumor Agents

Author(s): Romeo Romagnoli, Pier Giovanni Baraldi, Olga Cruz-Lopez, Carlota Lopez-Cara and Delia Preti

Volume 9, Issue 1, 2009

Page: [81 - 94] Pages: 14

DOI: 10.2174/138955709787001640

Price: $65


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.

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

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