Synthesis and antiproliferative activities against breast cancer of N-(benzimidazol-2-yl)-substituted benzamide derivatives

The strategic design of benzimidazole structures, akin to nucleotides, facilitates intricate interactions with amino acids within protein active sites.This structural scaffold, endowed with favorable pharmacokinetic profiles and lipophilic attributes, serves as a cornerstone in crafting potent pharmaceutical entities.In this study, a series of N-(1H-benzo[d]imidazol-2-yl)-substituted benzamides was meticulously synthesized and characterized through comprehensive spectroscopic analyses.Leveraging the established pharmacophoric role of substituted benzimidazoles, renowned for their documented anti-proliferative properties, this study embarked on the synthesis of benzamides employing methoxy and substituted phenyl rings as key pharmacophores, known for their anticancer efficacy.Subsequent cytotoxicity evaluations using the MTT assay against breast cancer (MCF7) and normal mouse fibroblasts (L929) revealed compound 9 as the leading candidate, inducing significant cytotoxicity.This suggests its potential as a potent anticancer agent through apoptotic pathways.These findings highlight compound 9 as a promising molecular scaffold that requires careful optimization for the development of effective anticancer therapies.

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Publication Details

Journal
Bioorganic & Medicinal Chemistry Reports
Published
2024-08-09
DOI
https://doi.org/10.25135/bmcr.32.24.03.3179
Primary Topic
Synthesis and biological activity
Type
article
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article

Synthesis and antiproliferative activities against breast cancer of N-(benzimidazol-2-yl)-substituted benzamide derivatives

Suat Çolak, Elif Akgöz
Bioorganic & Medicinal Chemistry Reports
Synthesis and biological activity
article

Synthesis and antiproliferative activities against breast cancer of N-(benzimidazol-2-yl)-substituted benzamide derivatives

Suat Çolak, Elif Akgöz
article en

Abstract

The strategic design of benzimidazole structures, akin to nucleotides, facilitates intricate interactions with amino acids within protein active sites.This structural scaffold, endowed with favorable pharmacokinetic profiles and lipophilic attributes, serves as a cornerstone in crafting potent pharmaceutical entities.In this study, a series of N-(1H-benzo[d]imidazol-2-yl)-substituted benzamides was meticulously synthesized and characterized through comprehensive spectroscopic analyses.Leveraging the established pharmacophoric role of substituted benzimidazoles, renowned for their documented anti-proliferative properties, this study embarked on the synthesis of benzamides employing methoxy and substituted phenyl rings as key pharmacophores, known for their anticancer efficacy.Subsequent cytotoxicity evaluations using the MTT assay against breast cancer (MCF7) and normal mouse fibroblasts (L929) revealed compound 9 as the leading candidate, inducing significant cytotoxicity.This suggests its potential as a potent anticancer agent through apoptotic pathways.These findings highlight compound 9 as a promising molecular scaffold that requires careful optimization for the development of effective anticancer therapies.

Bioorganic & Medicinal Chemistry Reports(1)
Erzincan Binali Yıldırım University (TR)
Good health and well-being
Openalex Percentile: Top 91%
Synthesis and biological activity
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Synthesis and antiproliferative activities against breast cancer of N-(benzimidazol-2-yl)-substituted benzamide derivatives — Suat Çolak, Elif Akgöz · Bioorganic & Medicinal Chemistry Reports (2024) | TGRS Research Map | TGRS