Synthesis of dendritic bisphosphonates as bone targeting ligands

Kazuma Shimoda, Takahiro Mitsuoka, Kenta Ueda, Hiroshi Suemune, Go Hirai, Mariko Aso

Research output: Contribution to journalArticle

1 Citation (Scopus)

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.

Original languageEnglish
Pages (from-to)4528-4531
Number of pages4
JournalTetrahedron Letters
Volume59
Issue number51
DOIs
Publication statusPublished - Dec 19 2018

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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