Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 93, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2023.129425
Keywords
Benzofuran; Piperazine; IPSO substitution; Necrosis; In vivo efficacy
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This work describes the synthesis and evaluation of potential anticancer agents, substituted benzofuran piperazines. The synthesized candidates were tested for their ability to inhibit cell proliferation in six different cancer cell lines. Furthermore, in vitro and in vivo evaluations revealed the lead compound's potential pathways for causing cell death and its effective anticancer efficacy in a MDA-MB-231 xenograft model.
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.
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