title: alpha-halogenoacrylic derivatives of antitumor agents.
abstract: In this review article we have reported a series of hybrid compounds characterized by the presence of a alpha-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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100-Ferrara, Italy. rmr@unife.it
authors.forename: Romeo
authors.initials: R
authors.lastname: Romagnoli
authors.forename: Pier Giovanni
authors.initials: PG
authors.lastname: Baraldi
authors.forename: Olga
authors.initials: O
authors.lastname: Cruz-Lopez
authors.forename: Carlota
authors.initials: C
authors.lastname: Lopez-Cara
authors.forename: Delia
authors.initials: D
authors.lastname: Preti
mesh_terms: D000818:Animals; D018906:Antineoplastic Agents, Alkylating / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004214:Distamycins / Q000737:chemistry / Q000494:pharmacology; D006146:Guanidines / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D051379:Mice; D011758:Pyrroles / Q000737:chemistry / Q000627:therapeutic use; D047608:Pyrroloiminoquinones / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D018906:Antineoplastic Agents, Alkylating; D004214:Distamycins; D006146:Guanidines; D011758:Pyrroles; D047608:Pyrroloiminoquinones; C030000:stallimycin; C455279:brostallicin