Pyrrolo[2,1-c][1,4]benzodiazepine as a Scaffold for the Design and Synthesis of Anti- Tumour Drugs

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Pyrrolo[2,1-c][1,4]benzodiazepine as a Scaffold for the Design and Synthesis of Anti- Tumour Drugs

Anti-Cancer Agents in Medicinal Chemistry, 9(1): 1-31.

Author(s): Laura Cipolla, Ana C. Araujo, Cristina Airoldi and Davide Bini.

Affiliation: Dept. of Biotechnology and Biosciences, University of Milano-Bicocca, P.zza della Scienza 2, 20126, Milano, Italy.


Compounds that bind in the minor groove of DNA have found use in the experimental treatment of cancer and certain infectious diseases. Furthermore, agents which target and can recognize discrete sequences of DNA have the potential to offer selective therapies by modulating the activity of specific transcription factors or genes. For this reason, a number of sequence-selective DNA binding agents have been evaluated with a range of affinities and recognition fidelities. In this respect, the pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) are of interest as they bind to guanine residues in the minor groove with a preference for Pu-G-Pu sequences. A dramatic increase in cytotoxicity and sequence selectivity has been achieved by linking two PBD units to form PBD dimers as cross-linking agents on opposite DNA strands (e.g., interstrand cross-links). SJG-136 is currently undergoing Phase I evaluation in both the United States (through the NCI) and United Kingdom (through Cancer Research United Kingdom). This review will focus on design, synthesis and structure activity relationship studies of pyrrolobenzodiazepines as anticancer therapeutics reported since 2003.


Anti- Tumour Drugs, Synthesis, pyrrolo[2,1-c][1,4]benzodiazepines (PBDs), transcription factors, cytotoxicity, PBD dimers, anticancer therapeutics.

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Article Details

Volume: 9
Issue Number: 1
First Page: 1
Last Page: 31
Page Count: 31
DOI: 10.2174/187152009787047743

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