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Exocyclic Sulfur and Selenoorganic Compounds Towards Their Anticancer Effects: Crystallographic and Biological

Ewa Żesławska1, Annamária Kincses2, Vivien Unger2

  • 1Department of Chemistry, Institute of Biology, Pedagogical University of Cracow, Kraków, Poland ewa.zeslawska@up.krakow.pl.

Anticancer Research
|August 1, 2018
PubMed
Abstract

Insights

New sulfur and selenium compounds show promise as anticancer agents. Sulfur analogues inhibit drug efflux, while selenium compounds exhibit potent cytotoxic and antiproliferative effects against mouse T-lymphoma cells.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Organic Chemistry

Background:

  • Multidrug resistance (MDR) presents significant challenges in cancer chemotherapy.
  • Developing novel anticancer agents and MDR inhibitors is crucial for improving treatment outcomes.

Purpose of the Study:

  • To evaluate the anticancer potential of novel exocyclic sulfur and selenoorganic compounds.
  • To assess their activity against mouse T-lymphoma cell lines, focusing on drug efflux modulation, cytotoxicity, and antiproliferative effects.

Main Methods:

  • Synthesis and evaluation of eighteen sulfur and selenium analogues of 2[1H]-pyrimidinone and hydantoin derivatives.
  • Assays for efflux modulation, cytotoxicity, and antiproliferation in mouse T-lymphoma cells.
  • Combination studies with doxorubicin on multidrug-resistant cells and crystal structure determination of key compounds.

Main Results:

  • Sulfur analogues with specific aromatic ring orientations demonstrated significant efflux inhibitory activity.
  • Selenium analogues exhibited notable antiproliferative and cytotoxic effects.
  • Two compounds with the highest efflux-modulating activity had their crystal structures determined.

Conclusions:

  • Sulfur analogues offer a scaffold for developing improved efflux inhibitors.
  • Selenium analogues show potential for enhancement in antiproliferative and cytotoxic activities.
  • These compounds represent promising leads for novel anticancer drug development.
Keywords:
P-gp inhibitorPyrimidinethioneantiproliferative activitycombination assay with doxorubicincrystal structurepyrimidineselenoneselenohydantointhiohydantoin

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