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

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.

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Publication Details

Journal
Discover Chemistry.
Published
2026-04-15
DOI
https://doi.org/10.1007/s44371-026-00662-0
Primary Topic
Synthesis of Organic Compounds
Type
article
Field-Weighted Citation Impact
0.00

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article

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

Drissa Sissouma, Aboudramane Koné, Adingra Francesco Kouassi, S eacute raphin Kati Coulibaly et al.
Discover Chemistry.
Synthesis of Organic Compounds
article

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

Drissa Sissouma, Aboudramane Koné, Adingra Francesco Kouassi, S eacute raphin Kati Coulibaly, Sylvain Collet
article en

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.

Discover Chemistry.Vol. 3(1)
Université Alassane Ouattara (CI), Université Jean Lorougnon Guédé (CI), Chimie et Interdisciplinarité, Synthèse, Analyse, Modélisation (FR), Université Félix Houphouët-Boigny (CI)
Université de Nantes
Good health and well-being
Openalex Percentile: Top 24%
Synthesis of Organic Compounds
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Synthesis and biological evaluation of benzimidazolyl phenylpropenones as selective anticancer agents in prostate colon and breast cancer models — Drissa Sissouma, Aboudramane Koné, et al. · Discover Chemistry. (2026) | TGRS Research Map | TGRS