2. Academic Validation
  3. Design and evaluation of 1,2,3-dithiazoles and fused 1,2,4-dithiazines as anti-cancer agents

Design and evaluation of 1,2,3-dithiazoles and fused 1,2,4-dithiazines as anti-cancer agents

  • Bioorg Med Chem Lett. 2021 Jul 1:43:128078. doi: 10.1016/j.bmcl.2021.128078.
Kaitlyn A Maffuid 1,  Maria Koyioni 2,  Chad D Torrice 1,  William A Murphy 1,  Heemaja K Mewada 1,  Panayiotis A Koutentis 2,  Daniel J Crona 3,  Christopher R M Asquith 4
Affiliations

Affiliations

  • 1 Division of Pharmacotherapy and Experimental Therapeutics, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • 2 Department of Chemistry, University of Cyprus, P. O. Box 20537, 1678 Nicosia, Cyprus.
  • 3 Division of Pharmacotherapy and Experimental Therapeutics, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • 4 Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA. Electronic address: chris.asquith@unc.edu.
PMID: 33951490 DOI: 10.1016/j.bmcl.2021.128078
Abstract

Heteroatom rich 1,2,3-dithiazoles are relatively underexplored in medicinal chemistry. We now report screening data on a series of structurally diverse 1,2,3-dithiazoles and electronically related 1,2,4-dithiazines with the aim of identifying interesting starting points for potential future optimisation. The 1,2,3-dithiazoles, were obtained via a number of different syntheses and screened on a series of Cancer cell lines. These included breast, bladder, prostate, pancreatic, chordoma and lung Cancer cell lines with an additional skin fibroblast cell line as a toxicity control. Several low single digit micromolar compounds with promising therapeutic windows were identified for breast, bladder and prostate Cancer. Furthermore, key structural features of 1,2,3-dithiazoles are discussed, that show encouraging scope for future refinement.

Keywords

1,2,3-Dithiazole; Bladder cancer; Breast cancer; Chordoma; Pancreatic cancer; Prostate cancer.

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