Bisphosphonates (BPs) are now the most widely used drugs for diseases associated with increased bone resorption, such as osteoporosis, and tumor bone diseases. A significant drawback of the BPs is their poor oral absorption that is enhanced by the presence of bile acid substituents in the bisphosphonate framework, with no toxic effects. A straightforward synthesis of bile acid-containing hydroxybisphosphonates and a full characterization of these pharmaceutically important molecules, including an evaluation of affinity and the mechanism of binding to hydroxyapatite, is presented. The biological activity of bile acid-containing bisphosphonate salts was determined using the neutral-red assay on the L929 cell line and primary cultures of osteoclasts. The bioactivity of the new compounds was found superior than bisphosphonates of established activity.
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|Titolo:||Synthesis, characterization and biological activity of hydroxyl-bisphosphonic analogs of bile acids|
|Data di pubblicazione:||2012|
|Citazione:||Synthesis, characterization and biological activity of hydroxyl-bisphosphonic analogs of bile acids / Bortolini, O; Fantin, G; Fogagnolo, M; Rossetti, S; Maiuolo, Loredana; DI POMPO, G; Avnet, S; Granchi, D.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 52(2012), pp. 221-229.|
|Appare nelle tipologie:||1.1 Articolo in rivista|