Frontiers in Pharmacology (Feb 2022)

Efficient Synthesis of 2,3′-Spirobi (Indolin)-2′-Ones and Preliminary Evaluation of Their Damage to Mitochondria in HeLa Cells

  • Huajie Li,
  • Huajie Li,
  • Zhenjie Yu,
  • Zhenjie Yu,
  • Haoyi Sun,
  • Haoyi Sun,
  • Bo Liu,
  • Bo Liu,
  • Xin Wang,
  • Xin Wang,
  • Zhe Shao,
  • Zhe Shao,
  • Meiling Wang,
  • Meiling Wang,
  • Weilin Xie,
  • Weilin Xie,
  • Xingang Yao,
  • Qingqiang Yao,
  • Qingqiang Yao,
  • Ying Zhi,
  • Ying Zhi

DOI
https://doi.org/10.3389/fphar.2021.821518
Journal volume & issue
Vol. 12

Abstract

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A novel formal (4 + 1) annulation between N-(o-chloromethyl)aryl amides and 3-chlorooxindoles through in situ generated aza-ortho-QMs with 3-chlorooxindoles is reported for the synthesis of a series of 2,3′-spirobi (indolin)-2′-ones in high yields. Under structured illumination microscopy, compound 3a is found to change the mitochondrial morphology and induce mitophagy pathway, which might then trigger mitophagy in cancer cells.

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