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<p>In this study, benzimidazolyl–phenylpropenone derivatives (<b>4a–h</b>) were synthesized and fully characterized using <sup>1</sup>H, <sup>13</sup>C NMR spectroscopy and High-Resolution Mass Spectrometry (HRMS). Their in vitro anticancer activity was evaluated against human cancer cell lines, including prostate (PC3), colon (CaCo2 and HCT-116), and breast (MDA-MB-231 and MCF-7) tumors, alongside normal human skin fibroblasts. All compounds demonstrated promising cytotoxic activity against the cancer cell lines, with IC<sub>50</sub> values ranging from 1.35 to 7.48 µM. Toxicity toward normal fibroblasts was very strong to moderate, with IC<sub>50</sub> values between 0.61 and 8.02 µM. Compared with reference compounds Roscovitine and Paclitaxel (Taxol<sup>®</sup>), several derivatives showed higher activity than Roscovitine, though generally less potent than Paclitaxel.</p><p>These findings position benzimidazolyl–phenylpropenones as promising scaffolds for the development of novel anticancer agents.</p> Graphical abstract <p></p>

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Synthesis and biological evaluation of benzimidazolyl phenylpropenones as selective anticancer agents in prostate colon and breast cancer models

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年4月15日

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  • Aboudramane Koné,
  • Adingra Francesco Kouassi,
  • Souleymane Coulibaly,
  • Drissa Sissouma,
  • Sylvain Collet

摘要

In this study, benzimidazolyl–phenylpropenone derivatives (4a–h) were synthesized and fully characterized using 1H, 13C NMR spectroscopy and High-Resolution Mass Spectrometry (HRMS). Their in vitro anticancer activity was evaluated against human cancer cell lines, including prostate (PC3), colon (CaCo2 and HCT-116), and breast (MDA-MB-231 and MCF-7) tumors, alongside normal human skin fibroblasts. All compounds demonstrated promising cytotoxic activity against the cancer cell lines, with IC50 values ranging from 1.35 to 7.48 µM. Toxicity toward normal fibroblasts was very strong to moderate, with IC50 values between 0.61 and 8.02 µM. Compared with reference compounds Roscovitine and Paclitaxel (Taxol®), several derivatives showed higher activity than Roscovitine, though generally less potent than Paclitaxel.

These findings position benzimidazolyl–phenylpropenones as promising scaffolds for the development of novel anticancer agents.

Graphical abstract