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

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Title: Synthesis and biological evaluation of benzimidazolyl phenylpropenones as selective anticancer agents in prostate colon and breast cancer models.
Authors: Koné, Aboudramane, Kouassi, Adingra Francesco, Coulibaly, Souleymane, Sissouma, Drissa, Collet, Sylvain
Source: Discover Chemistry; 4/15/2026, Vol. 3 Issue 1, p1-11, 11p
Subject Terms: Antineoplastic agent synthesis, Animal models of breast cancer, Antineoplastic agents, Benzimidazole derivatives, Colon cancer, Nuclear magnetic resonance spectroscopy, Cell-mediated cytotoxicity, Prostate cancer, Drug discovery, Paclitaxel, Breast cancer
Abstract: 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. [ABSTRACT FROM AUTHOR]
Copyright of Discover Chemistry is the property of Springer Nature and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
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  Label: Title
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  Data: Synthesis and biological evaluation of benzimidazolyl phenylpropenones as selective anticancer agents in prostate colon and breast cancer models.
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  Data: <searchLink fieldCode="AR" term="%22Koné%2C+Aboudramane%22">Koné, Aboudramane</searchLink><br /><searchLink fieldCode="AR" term="%22Kouassi%2C+Adingra+Francesco%22">Kouassi, Adingra Francesco</searchLink><br /><searchLink fieldCode="AR" term="%22Coulibaly%2C+Souleymane%22">Coulibaly, Souleymane</searchLink><br /><searchLink fieldCode="AR" term="%22Sissouma%2C+Drissa%22">Sissouma, Drissa</searchLink><br /><searchLink fieldCode="AR" term="%22Collet%2C+Sylvain%22">Collet, Sylvain</searchLink>
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  Data: Discover Chemistry; 4/15/2026, Vol. 3 Issue 1, p1-11, 11p
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  Data: <searchLink fieldCode="DE" term="%22Antineoplastic+agent+synthesis%22">Antineoplastic agent synthesis</searchLink><br /><searchLink fieldCode="DE" term="%22Animal+models+of+breast+cancer%22">Animal models of breast cancer</searchLink><br /><searchLink fieldCode="DE" term="%22Antineoplastic+agents%22">Antineoplastic agents</searchLink><br /><searchLink fieldCode="DE" term="%22Benzimidazole+derivatives%22">Benzimidazole derivatives</searchLink><br /><searchLink fieldCode="DE" term="%22Colon+cancer%22">Colon cancer</searchLink><br /><searchLink fieldCode="DE" term="%22Nuclear+magnetic+resonance+spectroscopy%22">Nuclear magnetic resonance spectroscopy</searchLink><br /><searchLink fieldCode="DE" term="%22Cell-mediated+cytotoxicity%22">Cell-mediated cytotoxicity</searchLink><br /><searchLink fieldCode="DE" term="%22Prostate+cancer%22">Prostate cancer</searchLink><br /><searchLink fieldCode="DE" term="%22Drug+discovery%22">Drug discovery</searchLink><br /><searchLink fieldCode="DE" term="%22Paclitaxel%22">Paclitaxel</searchLink><br /><searchLink fieldCode="DE" term="%22Breast+cancer%22">Breast cancer</searchLink>
– Name: Abstract
  Label: Abstract
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  Data: In this study, benzimidazolyl–phenylpropenone derivatives (4a–h) were synthesized and fully characterized using <superscript>1</superscript>H, <superscript>13</superscript>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<subscript>50</subscript> values ranging from 1.35 to 7.48 µM. Toxicity toward normal fibroblasts was very strong to moderate, with IC<subscript>50</subscript> values between 0.61 and 8.02 µM. Compared with reference compounds Roscovitine and Paclitaxel (Taxol<superscript>®</superscript>), 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. [ABSTRACT FROM AUTHOR]
– Name: Abstract
  Label:
  Group: Ab
  Data: <i>Copyright of Discover Chemistry is the property of Springer Nature and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.)
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RecordInfo BibRecord:
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        Value: 10.1007/s44371-026-00662-0
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      – Code: eng
        Text: English
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        PageCount: 11
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      – SubjectFull: Antineoplastic agent synthesis
        Type: general
      – SubjectFull: Animal models of breast cancer
        Type: general
      – SubjectFull: Antineoplastic agents
        Type: general
      – SubjectFull: Benzimidazole derivatives
        Type: general
      – SubjectFull: Colon cancer
        Type: general
      – SubjectFull: Nuclear magnetic resonance spectroscopy
        Type: general
      – SubjectFull: Cell-mediated cytotoxicity
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      – SubjectFull: Prostate cancer
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      – SubjectFull: Drug discovery
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      – SubjectFull: Paclitaxel
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      – SubjectFull: Breast cancer
        Type: general
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      – TitleFull: Synthesis and biological evaluation of benzimidazolyl phenylpropenones as selective anticancer agents in prostate colon and breast cancer models.
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            NameFull: Koné, Aboudramane
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            NameFull: Kouassi, Adingra Francesco
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            – D: 15
              M: 04
              Text: 4/15/2026
              Type: published
              Y: 2026
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