☆ 4.7 Article

Effective synthesis of benzimidazoles-imidazo[1,2-a]pyrazine conjugates: A comparative study of mono-and bis-benzimidazoles for antitumor activity

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

卷 180, 期 -, 页码 546-561

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

DOI: 10.1016/j.ejmech.2019.07.042

关键词

Imidazo[1,2-a]pyrazine; Benzimidazole; Anticancer activity; DNA interaction; Bovine serum albumin

类别

Chemistry, Medicinal

资金

SERB, New Delhi [CRG/2018/002159]
CSIR [09/677(0033)/2018-EMR-I]

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Protocol

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摘要

A novel series of 6-substituted-8-(1-cyclohexyl-1H-benzo[d]imidazole-6-yl)imidazo[1,2-a]pyrazine and 6-substituted-8-(1-benzyl-1H-benzo[d]imidazole-6-yl)imidazo[1,2-a]pyrazine is first time synthesized and screen in vitro biological activity for 60 human cancer cell lines representing nine different cancer types. Derivatives 10 and 36 show antitumor activity for all tested cell lines, display comparable full panel mean-graph midpoint growth inhibition (MG_MID GI(50)) values of 2.10 and 2.23 mu M, respectively. Furthermore, these derivatives show strong binding interactions with DNA and bovine serum albumin (BSA), studied through absorption, emission, and circular dichroism techniques. These spectroscopic studies reveal that imidazo[1,2-a]pyrazine-benzimidazoles 10 and 36, intercalate with ct-DNA as a leading interaction for fundamental biologically significant effects, with monobenzimidazole show better activity than bisbenzimidazole. These experiments have confirmed that the imidazo[1,2-a]pyrazine and benzimidazole moieties are efficient pharmacophores to trigger binding to DNA. These compounds have also interacted with bovine serum albumin protein that demonstrating high values of binding constant. (C) 2019 Elsevier Masson SAS. All rights reserved.

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