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DNA binders in clinical trials and chemotherapy

Ali, Asfa and Bhattacharya, Santanu (2014) DNA binders in clinical trials and chemotherapy. In: BIOORGANIC & MEDICINAL CHEMISTRY, 22 (16). pp. 4506-4521.

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Official URL: http://dx.doi.org/ 10.1016/j.bmc.2014.05.030


Cancer has always been a dreadful disease and continues to attract extensive research investigations. Various targets have been identified to restrain cancer. Among these DNA happens to be the most explored one. A wide variety of small molecules, often referred to as `ligands', has been synthesized to target numerous structural features of DNA. The sole purpose of such molecular design has been to interfere with the transcriptional machinery in order to drive the cancer cell toward apoptosis. The mode of action of the DNA targeting ligands focuses either on the sequence-specificity by groove binding and strand cleavage, or by identifying the morphologically distinct higher order structures like that of the G-quadruplex DNA. However, in spite of the extensive research, only a tiny fraction of the molecules have been able to reach clinical trials and only a handful are used in chemotherapy. This review attempts to record the journey of the DNA binding small molecules from its inception to cancer therapy via various modifications at the molecular level. Nevertheless, factors like limited bioavailability, severe toxicities, unfavorable pharmacokinetics etc. still prove to be the major impediments in the field which warrant considerable scope for further research investigations. (C) 2014 Published by Elsevier Ltd.

Item Type: Journal Article
Additional Information: Copy right for this article belongs to the PERGAMON-ELSEVIER SCIENCE LTD, THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND
Keywords: Duplex DNA; G-quadruplex DNA; DNA binders; Topoisomerase; Chemotherapy; Clinical trials; Anticancer
Department/Centre: Division of Chemical Sciences > Organic Chemistry
Date Deposited: 24 Sep 2014 05:50
Last Modified: 24 Sep 2014 05:50
URI: http://eprints.iisc.ac.in/id/eprint/49930

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