title: Distamycins: strategies for possible enhancement of activity and specificity.
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.
authors.affiliation: CoReS Techno Group, Department of Pharmaceutical Sciences, University of Ferrara, BioPharmaNet, 44121 Ferrara, Italy. crt@unife.it
authors.forename: Rita
authors.initials: R
authors.lastname: Cortesi
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Esposito
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D004214:Distamycins / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D006571:Heterocyclic Compounds / Q000737:chemistry; D008081:Liposomes / Q000737:chemistry; D009588:Nitrogen Mustard Compounds / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D000998:Antiviral Agents; D004214:Distamycins; D006571:Heterocyclic Compounds; D008081:Liposomes; D009588:Nitrogen Mustard Compounds; C066900:tallimustine