Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5837
Title: 2-Hydroxypropyl-β-cyclodextrin strongly improves water solubility and anti-proliferative activity of pyrazolo[3,4-d]pyrimidines Src-Abl dual inhibitors.
Authors: Dreassi, Elena 
Zizzari, ALESSANDRA TANIA
Mori, Mattia 
Filippi, Irene
Belfiore, Amalia
Naldini, Antonella
Carraro, Fabio
Santucci, Annalisa 
Schenone, S
Botta, Maurizio 
Issue Date: 2010
Project: None 
Journal: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Abstract: 
The main aim of this study was to enhance the solubility of pyrazolo[3,4-d]pyrimidines 1-8 able to strongly inhibit Src and Abl tyrosine kinase phosphorylation in cell-free assays and to significantly reduce leukemic and osteosarcoma cell lines growth, but characterized by very low solubility in aqueous media. Their water solubility was improved between 100 and 1000 folds by solubilization with 2-hydroxypropyl-β-cyclodextrin (HPβCD) and ratio of inclusion complex were determined by phase solubility method. Finally, some complexed compounds were tested on different leukemic (K-652, KU-812 and HL-60) and osteosarcoma (SaOS-2) cell lines showing a good enhancement of biological response in comparison with the not complexed compounds.
Description: 
35633
URI: http://hdl.handle.net/20.500.12779/5837
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2010.09.062
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