Scholarlink

<p>This current study explores the synthesis and anticancer efficacy of novel Pirfenidone related molecules targeting the MCF7 breast cancer cell line. A series of Pirfenidone derivatives (PA1-6) were designed and synthesized. Initial computational analyses, including pharmacokinetic profiling and docking screenings, were executed to evaluate the interaction of these derivatives with VEGFR-2 kinase, a crucial target in cancer progression. Following in silico explorations, the synthesized derivatives underwent in vitro testing to determine their cytotoxic effects and establish IC<sub>50</sub> values. Results indicated that the derivatives exhibited varying levels of efficacy, with PA2 demonstrating the highest potency (IC<sub>50</sub> = 15.25 ± 3.02&#xa0;µM). Structure–activity relationship (SAR) analysis highlighted the influence of substituents on the phenyl ring in modulating anticancer activity. Additionally, flow cytometry analysis suggested that PA2 induces apoptosis in the S phase of the cell cycle. Overall study underscores the therapeutic potential of Pirfenidone derivatives as promising candidates for breast cancer treatment.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Design, synthesis, and biological evaluation of pirfenidone-based compounds against breast cancer

  • 期刊论文

  • 发表日期：

    2025年11月20日

查看全文
  • Raghavendra Hegde,
  • Itte Pushpavathi,
  • B. N. Nippu,
  • T. M. Madhukumar

摘要

This current study explores the synthesis and anticancer efficacy of novel Pirfenidone related molecules targeting the MCF7 breast cancer cell line. A series of Pirfenidone derivatives (PA1-6) were designed and synthesized. Initial computational analyses, including pharmacokinetic profiling and docking screenings, were executed to evaluate the interaction of these derivatives with VEGFR-2 kinase, a crucial target in cancer progression. Following in silico explorations, the synthesized derivatives underwent in vitro testing to determine their cytotoxic effects and establish IC50 values. Results indicated that the derivatives exhibited varying levels of efficacy, with PA2 demonstrating the highest potency (IC50 = 15.25 ± 3.02 µM). Structure–activity relationship (SAR) analysis highlighted the influence of substituents on the phenyl ring in modulating anticancer activity. Additionally, flow cytometry analysis suggested that PA2 induces apoptosis in the S phase of the cell cycle. Overall study underscores the therapeutic potential of Pirfenidone derivatives as promising candidates for breast cancer treatment.