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 17, 14 Issues, 2017


Download PDF Flyer




Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

This journal supports open access

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 27th of 59 in Chemistry, Medicinal

Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
ICCF-CNRS UMR 6296
Université Clermont Auvergne
Clermont-Ferrand
France


View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.722
5 - Year: 2.849

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.

Abstract

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.

Keywords:

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



Download Free Order Reprints Order Eprints Rights and Permissions




Article Details

Volume: 9
Issue Number: 1
First Page: 1
Last Page: 31
Page Count: 31
DOI: 10.2174/187152009787047743
Advertisement
Global Biotechnology Congress 2017Drug Discovery and Therapy World Congress 2017

Related Journals




Related eBooks



Webmaster Contact: urooj@benthamscience.org Copyright © 2017 Bentham Science