Abstract
The present review focused on the strategies aimed to possibly solve toxicity problems of distamycins. Distamycins are compounds characterized by an oligopeptidic pyrrolocarbamoyl frame ending with an amidino moiety. This class of compounds displays antiviral and antibiotic activity and shows interesting antiprotozoal activity related to the ability to reversibly bind to the minor groove of DNA with a high selectivity for TA-rich sequences. In consideration of their potential therapeutic properties, the synthesis of new distamycin derivatives and especially the development of controlled delivery strategies, could lead to important advantages in the clinical use of these molecules, possibly overcoming or mitigating the low solubility, specificity and toxicity problems associated with their use. To these aims an ensemble of the main synthetic distamycin derived compounds and of the potential drug delivery systems for distamycins described in literature is reviewed.
Keywords: Liposomes, distamycins, antiproliferative activity, antitumor drugs
Mini-Reviews in Medicinal Chemistry
Title: Distamycins: Strategies for Possible Enhancement of Activity and Specificity
Volume: 10 Issue: 3
Author(s): Rita Cortesi and Elisabetta Esposito
Affiliation:
Keywords: Liposomes, distamycins, antiproliferative activity, antitumor drugs
Abstract: The present review focused on the strategies aimed to possibly solve toxicity problems of distamycins. Distamycins are compounds characterized by an oligopeptidic pyrrolocarbamoyl frame ending with an amidino moiety. This class of compounds displays antiviral and antibiotic activity and shows interesting antiprotozoal activity related to the ability to reversibly bind to the minor groove of DNA with a high selectivity for TA-rich sequences. In consideration of their potential therapeutic properties, the synthesis of new distamycin derivatives and especially the development of controlled delivery strategies, could lead to important advantages in the clinical use of these molecules, possibly overcoming or mitigating the low solubility, specificity and toxicity problems associated with their use. To these aims an ensemble of the main synthetic distamycin derived compounds and of the potential drug delivery systems for distamycins described in literature is reviewed.
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Cortesi Rita and Esposito Elisabetta, Distamycins: Strategies for Possible Enhancement of Activity and Specificity, Mini-Reviews in Medicinal Chemistry 2010; 10 (3) . https://dx.doi.org/10.2174/138955710791185055
DOI https://dx.doi.org/10.2174/138955710791185055 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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