Design, synthesis and biological activity of a pyrrolo [2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid.
We report the synthesis of a new hybrid 13 which is a combination of the naturally occurring antitumor agent distamycin A 1 and the pyrrolo[2,1-c][1,4]benzodiazepine 11, related to the naturally occurring anthramycin 2. The antitumor activity of the hybrid 13 was tested in vitro and compared to the natural product distamycin 1 and the PBD 11.
Baraldi
P G
PG
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy. pgb@dns.unife.it
Cacciari
B
B
Guiotto
A
A
Leoni
A
A
Romagnoli
R
R
Spalluto
G
G
Mongelli
N
N
Howard
P W
PW
Thurston
D E
DE
Bianchi
N
N
Gambari
R
R
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D004247:DNA / Q000378:metabolism; D004214:Distamycins / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D020014:K562 Cells; D016133:Polymerase Chain Reaction
D000970:Antineoplastic Agents; D004214:Distamycins; D001569:Benzodiazepines; C030000:stallimycin; D004247:DNA