1-[3-(2-Hydroxyethylsulfanyl)propanoyl]-3,5-bis(benzylidene)-4-piperidones: A novel cluster of P-glycoprotein dependent multidrug resistance modulators

Umashankar Das, Hari N. Pati, Zoltan Baráth, Ákos Csonka, J. Molnár, Jonathan R. Dimmock

Research output: Contribution to journalArticle

3 Citations (Scopus)


A series of 1-[3-(2-hydroxyethylsulfanyl)propanoyl]-3,5-bis(benzylidene)-4-piperidones 4a-e display promising P-glycoprotein dependent multidrug resistance (MDR) revertant properties and are significantly more potent than a reference drug verapamil when evaluated against L-5178Y MDR lymphoma cells. These dienones may be referred to as dual agents having both MDR revertant properties and tumour-selective cytotoxicity. In particular, 3,5-bis(4-chlorobenzylidene)-1-[3-(2-hydroxyethylsulfanyl]propanoyl-4-piperidone 4d emerged as a lead molecule for further development based on its MDR revertant properties, cytotoxic potencies and tumour-selective toxicity. The structure-activity relationships reveal important structural requirements for further designing of potent MDR revertants. 2016 Elsevier Ltd. All rights reserved.

Original languageEnglish
Pages (from-to)1319-1321
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Issue number4
Publication statusPublished - Feb 15 2016


  • 3,5-Bis(benzylidene)-4-piperidones
  • MDR revertants
  • P-glycoprotein
  • Selective cytotoxicity
  • Structure-activity relationships

ASJC Scopus subject areas

  • Biochemistry
  • Clinical Biochemistry
  • Molecular Biology
  • Molecular Medicine
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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