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Updated: Dec 18, 2025

Synthesis of 1,2-Azaborines and the Preparation of Their Protein Complexes with T4 Lysozyme Mutants
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Synthesis and biological evaluation of arylphosphonium-benzoxaborole conjugates as novel anticancer agents

Sravan K Jonnalagadda1, Kevin Wielenberg2, Conor T Ronayne1

  • 1Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA.

Bioorganic & Medicinal Chemistry Letters
|June 13, 2020
PubMed

Insights

New arylphosphonium-benzoxaborole conjugates show promise as mitochondria-targeting anticancer agents. Lead compound 6c effectively reduced cancer cell viability and inhibited mitochondrial respiration.

Area of Science:

  • Medicinal Chemistry
  • Cancer Biology
  • Mitochondrial Biology

Background:

  • Mitochondria are crucial targets for anticancer drug development.
  • Arylphosphonium-benzoxaborole conjugates offer a novel scaffold for drug design.

Purpose of the Study:

  • To synthesize and evaluate arylphosphonium-benzoxaborole conjugates as mitochondria-targeting anticancer agents.
  • To identify a lead compound for further preclinical development.

Main Methods:

  • Synthesis of arylphosphonium-benzoxaborole conjugates.
  • In vitro cell viability assays on breast, pancreatic, and colorectal cancer cell lines.
  • Seahorse Xfe96 metabolic assays to assess mitochondrial respiration.
  • Epifluorescent microscopy to evaluate mitochondrial morphology.

Main Results:

  • Compound 6c demonstrated significant cytotoxicity across multiple solid tumor cell lines.
  • Lead compound 6c inhibited mitochondrial respiration, reducing ATP production and increasing proton leak in 4T1 and WiDr cells.
  • 6c induced mitochondrial fragmentation, indicative of programmed cell death.

Conclusions:

  • Arylphosphonium-benzoxaborole conjugates represent a promising class of mitochondria-targeting anticancer agents.
  • Compound 6c warrants further investigation as a potential therapeutic candidate for solid tumors.
Keywords:
BenzoxaboroleCell viabilityGlycolysis stress testMitochondrial fragmentationMitochondrial stress testPhosphonium salts

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