Synthesis of Melphalan-Gem-Bisphosphonate Conjugation to Bone Tumors and Study of Affinity to Hydroxyapatite In Vitro

Qinglin      Jiang; Li      Yang; Li      Hai; Yong      Wu

doi:10.2174/157017808783955862

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

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Letters in Organic Chemistry

Title: Synthesis of Melphalan-Gem-Bisphosphonate Conjugation to Bone Tumors and Study of Affinity to Hydroxyapatite In Vitro

Volume: 5 Issue: 3

Author(s): Qinglin Jiang, Li Yang, Li Hai and Yong Wu

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

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.

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Jiang Qinglin, Yang Li, Hai Li and Wu Yong, Synthesis of Melphalan-Gem-Bisphosphonate Conjugation to Bone Tumors and Study of Affinity to Hydroxyapatite In Vitro, Letters in Organic Chemistry 2008; 5 (3) . https://dx.doi.org/10.2174/157017808783955862