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  3. Synthesis and biological evaluation of benzofuran piperazine derivatives as potential anticancer agents

Synthesis and biological evaluation of benzofuran piperazine derivatives as potential anticancer agents

  • Bioorg Med Chem Lett. 2023 Sep 1:93:129425. doi: 10.1016/j.bmcl.2023.129425.
Tanner J Schumacher 1,  Naresh Sah 2,  Komaraiah Palle 2,  Jon Rumbley 3,  Venkatram R Mereddy 4
Affiliations

Affiliations

  • 1 Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, United States.
  • 2 Department of Cell Biology and Biochemistry, Texas Tech University Health Sciences Center, Lubbock, TX 79430, United States.
  • 3 Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, United States; Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota, Duluth, MN 55812, United States.
  • 4 Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, United States; Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota, Duluth, MN 55812, United States; Department of Chemistry and Biochemistry, University of Minnesota Duluth, Duluth, MN 55812, United States. Electronic address: [email protected].
PMID: 37557926 DOI: 10.1016/j.bmcl.2023.129425
Abstract

This work describes about the synthesis and evaluation of substituted benzofuran piperazines as potential Anticancer agents. The synthesized candidates have been evaluated for their cell proliferation inhibition properties in six murine and human Cancer cell lines. In vitro evaluation of Apoptosis and cell cycle analysis with the lead candidate 1.19 reveals that necrosis might be an important pathway for the candidate compounds to cause cell death. Further, in vivo evaluation of the lead compound shows that this candidate is well tolerated in healthy mice. Additionally, an in vivo Anticancer efficacy study in mice using a MDA-MB-231 xenograft model with the lead compound provides good anti-cancer efficacy.

Keywords

Benzofuran; IPSO substitution; In vivo efficacy; Necrosis; Piperazine.

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