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

Tanner J. Schumacher, Naresh Sah, Komaraiah Palle, Jon Rumbley, Venkatram R. Mereddy

Research output: Contribution to journalArticlepeer-review

11 Scopus citations

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.

Original languageEnglish (US)
Article number129425
JournalBioorganic and Medicinal Chemistry Letters
Volume93
DOIs
StatePublished - Sep 1 2023

Bibliographical note

Publisher Copyright:
© 2023 Elsevier Ltd

Keywords

  • Benzofuran
  • IPSO substitution
  • In vivo efficacy
  • Necrosis
  • Piperazine

PubMed: MeSH publication types

  • Journal Article
  • Research Support, Non-U.S. Gov't

Fingerprint

Dive into the research topics of 'Synthesis and biological evaluation of benzofuran piperazine derivatives as potential anticancer agents'. Together they form a unique fingerprint.

Cite this