Benzazole–Carboxamide Hybrids as Potent Antiproliferative Agents Against Breast Cancer Cells

Breast cancer remains a leading cause of cancer-related mortality worldwide, and the development of novel small-molecule agents with improved efficacy and selectivity is still urgently needed. Although benzazole and benzamide scaffolds are individually recognized for their diverse pharmacological activities, systematic studies exploring hybrid N-(benzazol-2-yl)4-substituted benzamide derivatives as antiproliferative agents against breast cancer are limited. In this study, a series of N-(benzazol-2-yl)-4-substituted benzamide derivatives was synthesized and fully characterized by ¹H NMR, ¹³C NMR, and IR spectroscopy. The antiproliferative activities of the synthesized compounds were evaluated against the human breast cancer cell line MCF-7 and the normal fibroblast cell line L929 using the MTT assay. The compounds were obtained in good to excellent yields (70–85%). Several derivatives exhibited strong growth-inhibitory effects, with IC₅₀ values ranging from 3.11 to 12.39 µM. Among the tested molecules, compounds 6 and 11 demonstrated the most significant cytotoxic effects, and compound 6 emerged as the most promising candidate for further investigation. These findings provide preliminary structure–activity insights and highlight benzazole–benzamide hybrids as promising scaffolds for further anticancer drug development.

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Publication Details

Journal
EMU Journal of Pharmaceutical Sciences
Published
2026-05-21
DOI
https://doi.org/10.54994/emujpharmsci.1838511
Primary Topic
Synthesis and biological activity
Type
article
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article

Benzazole–Carboxamide Hybrids as Potent Antiproliferative Agents Against Breast Cancer Cells

Ronak Haj Ersan, Omer Faruk Col, Şule Gürsoy
EMU Journal of Pharmaceutical Sciences
Synthesis and biological activity
article

Benzazole–Carboxamide Hybrids as Potent Antiproliferative Agents Against Breast Cancer Cells

Ronak Haj Ersan, Omer Faruk Col, Şule Gürsoy
article en

Abstract

Breast cancer remains a leading cause of cancer-related mortality worldwide, and the development of novel small-molecule agents with improved efficacy and selectivity is still urgently needed. Although benzazole and benzamide scaffolds are individually recognized for their diverse pharmacological activities, systematic studies exploring hybrid N-(benzazol-2-yl)4-substituted benzamide derivatives as antiproliferative agents against breast cancer are limited. In this study, a series of N-(benzazol-2-yl)-4-substituted benzamide derivatives was synthesized and fully characterized by ¹H NMR, ¹³C NMR, and IR spectroscopy. The antiproliferative activities of the synthesized compounds were evaluated against the human breast cancer cell line MCF-7 and the normal fibroblast cell line L929 using the MTT assay. The compounds were obtained in good to excellent yields (70–85%). Several derivatives exhibited strong growth-inhibitory effects, with IC₅₀ values ranging from 3.11 to 12.39 µM. Among the tested molecules, compounds 6 and 11 demonstrated the most significant cytotoxic effects, and compound 6 emerged as the most promising candidate for further investigation. These findings provide preliminary structure–activity insights and highlight benzazole–benzamide hybrids as promising scaffolds for further anticancer drug development.

EMU Journal of Pharmaceutical SciencesVol. 9(1)
Cihan University-Erbil (IQ), Gazi Hastanesi (TR)
Good health and well-being
Openalex Percentile: Top 10%
Synthesis and biological activity
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