Scholarlink

<p>A new series of conjugates linking 5-FU with parts of pterostilbene and biphenyl were designed, and synthesized, besides, their biological activity was assessed against human colorectal adenocarcinoma cells (SW480) and the non-malignant cell line NCM460. Novel conjugates were first screened to establish the potential at 100 µM single dose, finding two active compounds <b>5e</b> and <b>5g</b> that caused more than 70% inhibition. In addition, in the seven-dose screening it was observed that, although both compounds were more active than the starting molecule <b>3</b>, only compound <b>5e</b> was more selective toward cancer cells than the drug 5-fluorouracil (5-FU). A theoretical examination of pharmacokinetics, toxicological, and drug-like characteristics indicates that the most promising hybrid <b>5e</b>, has a strong potential to progress to further preclinical studies. Our findings unequivocally showed the effectiveness of 5-FU/pterostilbene hybrids, with the 3,4,5-trimethoxyphenylsubstituted compound serving as a prototype molecule for upcoming studies that focus on new methods for treating colorectal cancer.</p><p></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

Discovery of novel pterostilbene/biphenyl tethered 5-FU based conjugates targeting colorectal cancer: synthesis, cytotoxic and ADMET modeling studies

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年4月15日

查看全文
  • Rubén Becerra-Quintana,
  • Angie Herrera-Ramírez,
  • Andrés F. Yepes,
  • Laura Cadavid-Arango,
  • Wilson Cardona-Galeano

摘要

A new series of conjugates linking 5-FU with parts of pterostilbene and biphenyl were designed, and synthesized, besides, their biological activity was assessed against human colorectal adenocarcinoma cells (SW480) and the non-malignant cell line NCM460. Novel conjugates were first screened to establish the potential at 100 µM single dose, finding two active compounds 5e and 5g that caused more than 70% inhibition. In addition, in the seven-dose screening it was observed that, although both compounds were more active than the starting molecule 3, only compound 5e was more selective toward cancer cells than the drug 5-fluorouracil (5-FU). A theoretical examination of pharmacokinetics, toxicological, and drug-like characteristics indicates that the most promising hybrid 5e, has a strong potential to progress to further preclinical studies. Our findings unequivocally showed the effectiveness of 5-FU/pterostilbene hybrids, with the 3,4,5-trimethoxyphenylsubstituted compound serving as a prototype molecule for upcoming studies that focus on new methods for treating colorectal cancer.