alpha-halogenoacrylic derivatives of antitumor agents.
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.
Romagnoli
Romeo
R
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100-Ferrara, Italy. rmr@unife.it
Baraldi
Pier Giovanni
PG
Cruz-Lopez
Olga
O
Lopez-Cara
Carlota
C
Preti
Delia
D
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
D018906:Antineoplastic Agents, Alkylating; D004214:Distamycins; D006146:Guanidines; D011758:Pyrroles; D047608:Pyrroloiminoquinones; C030000:stallimycin; C455279:brostallicin