Design, synthesis and biological activity of a pyrrolo [2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid

P G Baraldi; B Cacciari; A Guiotto; A Leoni; R Romagnoli; G Spalluto; N Mongelli; P W Howard; D E Thurston; N Bianchi; R Gambari

doi:10.1016/S0960-894X(98)00544-7

Design, synthesis and biological activity of a pyrrolo [2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid

Bioorg Med Chem Lett. 1998 Nov 3;8(21):3019-24. doi: 10.1016/S0960-894X(98)00544-7.

Authors

P G Baraldi¹, B Cacciari, A Guiotto, A Leoni, R Romagnoli, G Spalluto, N Mongelli, P W Howard, D E Thurston, N Bianchi, R Gambari

Affiliation

¹ Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy. pgb@dns.unife.it

PMID: 9873668
DOI: 10.1016/S0960-894X(98)00544-7

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / metabolism
Antineoplastic Agents / pharmacology
Benzodiazepines / chemical synthesis*
Benzodiazepines / metabolism
Benzodiazepines / pharmacology
DNA / metabolism
Distamycins / chemical synthesis*
Distamycins / metabolism
Distamycins / pharmacology
Drug Design*
Humans
K562 Cells
Polymerase Chain Reaction

Substances

Antineoplastic Agents
Distamycins
Benzodiazepines
stallimycin
DNA