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The development of pyrrolobenzodiazepines as antitumour agents

Hartley, JA; (2011) The development of pyrrolobenzodiazepines as antitumour agents. EXPERT OPIN INV DRUG , 20 (6) 733 - 744. 10.1517/13543784.2011.573477.

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Abstract

Introduction: DNA interacting agents play a major role in cancer chemotherapy, either as single agents, in combination drug regimens, or as components of novel targeted therapies. The search for more selective and efficacious drugs that can deliver critical DNA damage with minimal side effects continues.Areas covered: The development of the pyrrolobenzodiazepines (PBDs) from their discovery as natural products in the 1960s, through synthetic PBD monomers, PBD hybrids and conjugates, and PBD dimers is described. The latter molecules are capable of forming sequence selective, non-distorting and potently cytotoxic DNA interstrand cross-links in the minor groove of DNA. In particular, the development of PBD dimer SJG-136 (SG2000), currently in Phase II clinical trials, is presented. Potential future cancer therapeutic applications of PBDs, including their use as components of targeting strategies, are also discussed.Expert opinion: The culmination of over four decades of study on structure--activity relationships of PBDs has led to a detailed understanding of how to introduce structural modification to enhance biological activity and potency. The challenge for the next phase in the development of the PBDs is to harness this activity and potency in a new generation of cancer therapeutics.

Type: Article
Title: The development of pyrrolobenzodiazepines as antitumour agents
DOI: 10.1517/13543784.2011.573477
Keywords: antitumour agent, DNA cross-linking agent, DNA interacting agents, DNA minor groove binding drugs, PBD, pyrrolobenzodiazepine, SG2000, SJG-136, CROSS-LINKING AGENT, LYMPHOCYTIC-LEUKEMIA CELLS, DNA-BINDING PROPERTIES, ADVANCED SOLID TUMORS, SJG-136 NSC-694501, IN-VITRO, MAMMALIAN-CELLS, PRECLINICAL PHARMACOLOGY, CHEMOTHERAPEUTIC-AGENTS, CELLULAR PHARMACOLOGY
UCL classification: UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Cancer Institute
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Cancer Institute > Research Department of Oncology
URI: http://discovery.ucl.ac.uk/id/eprint/1302915
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