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

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.