Abstract

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