Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, United States.
Department of Cell Biology and Biochemistry, Texas Tech University Health Sciences Center, Lubbock, TX 79430, United States.
Bioorg Med Chem Lett. 2023 Sep 1;93:129425. doi: 10.1016/j.bmcl.2023.129425. Epub 2023 Aug 7.
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.
本工作描述了取代苯并呋喃哌嗪类化合物的合成和评估，作为潜在的抗癌剂。合成的候选物已在六种鼠和人癌细胞系中评估了它们的细胞增殖抑制特性。用先导化合物 1.19 进行的体外凋亡和细胞周期分析评估表明，坏死可能是候选化合物引起细胞死亡的重要途径。此外，在健康小鼠中的体内评价表明，该候选物具有良好的耐受性。此外，用先导化合物在 MDA-MB-231 异种移植模型中进行的体内抗癌功效研究在小鼠中提供了良好的抗癌功效。
