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 language | English (US) |
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Article number | 129425 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 93 |
DOIs | |
State | Published - 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