Abstract

To develop a methodology for bone-specific delivery of drugs, a bone-targeting gem-bisphosphonate was used as a carrier of drugs. We had synthesized five compounds, which were a new class of potential bone-targeting reagents for bone tumors consisting of melphalan linked to a gem-bisphosphonate moiety through an amide linkage. The conjugates showed a high affinity to hydroxyapatite in vitro.

Keywords: Bone-targeting, gem-bisphosphonates, melphalan, bone tumors