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Abstract <p>The reaction of indole-3-glyoxylyl chloride with α,ω-azidoalkanols and α,ω-azidoalkylamines afforded azide analogues of indibulin. The latter were reacted with acetylene derivatives of 3,5-bis(benzylidene)piperidin-4-ones using click chemistry approaches. The resulting conjugates were tested for antiproliferative activity.</p>

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Design of Cytotoxic Conjugates of Indole-3-glyoxylamides and 3,5-Bis(benzylidene)piperidin-4-ones by Click Chemistry Using Molecular Hybridization Strategy

  • 期刊论文

  • 发表日期：

    2026年7月23日

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  • Elena V. Sharova,
  • Oleg I. Artyushin,
  • Ekaterina V. Smirnova,
  • Inna A. Shagina,
  • Yulia R. Aleksandrova,
  • Margarita E. Neganova,
  • Valery K. Brel

摘要

Abstract

The reaction of indole-3-glyoxylyl chloride with α,ω-azidoalkanols and α,ω-azidoalkylamines afforded azide analogues of indibulin. The latter were reacted with acetylene derivatives of 3,5-bis(benzylidene)piperidin-4-ones using click chemistry approaches. The resulting conjugates were tested for antiproliferative activity.