Synthesis of dendritic bisphosphonates as bone targeting ligands |
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| Authors: | Kazuma Shimoda Takahiro Mitsuoka Kenta Ueda Hiroshi Suemune Go Hirai Mariko Aso |
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| Affiliation: | 1. Faculty of Pharmaceutical Sciences, Kyushu University, 3-1-1, Maidashi, Higashi-ku, Fukuoka 812-8582, Japan;2. Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1, Maidashi, Higashi-ku, Fukuoka 812-8582, Japan |
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| Abstract: | A dendritic bisphosphonate carrying three bisphosphonate (BP) units in close proximity was designed as a ligand to conjugate large therapeutic molecules for their bone selective delivery. The Bu3P-catalyzed conjugate addition of nitromethane to vinylidene bisphosphonate was effective to construct a quaternary carbon center carrying BP units. Owing to multivalent interactions, the dendritic bisphosphonate showed considerable affinity for the bone mineral hydroxyapatite even in the presence of a competitor, demonstrating potential as a bone targeting ligand. |
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| Keywords: | Bisphosphonate Bone targeting Conjugate Multivalent interaction |
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