Antiviral and Antiproliferative Activity <i>in vitro</i> of some New Benzimidazole Derivatives

Castelli, M; Malagoli, M; Lupo, Lucia; Riccomi, Tiziana Rossi; Casolari, Chiara; Cermelli, Claudio; Zanca, Andrea; Baggio, Giosué

doi:10.1034/j.1600-0773.2001.088002067.x

Cited by 10 publications

(5 citation statements)

References 15 publications

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“…Benzothiazoles are heterocyclic compounds and they structurally look like DNA purine bases (Castelli et al, 2001). They have been investigated for antitumor, antimicrobial, antifungal, and antimalarial activities (Soni et al, 2010;Saeed et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Benzothiazole derivatives as human DNA topoisomerase IIα inhibitors

et al. 2013

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Benzothiazole derivatives resembling the structure of DNA purine bases were tested to determine their topoisomerase inhibition activities. Based on DNA topoisomerase I and II relaxation assay results, all 12 derivatives acted as human topoisomerase IIa inhibitors, whereas only two compounds inhibited Calf thymus topoisomerase I. 3-amino-2-(2-bromobenzyl)-1,3-benzothiazol-3-ium 4-methylbenzensulfonate (BM3) was observed to be the most effective human topoisomerase IIa inhibitor with the lowest IC 50 value of 39 nM. The mechanistic studies suggested that BM3 was neither a DNA intercalator nor a topoisomerase poison, it was only a DNA minor groovebinding agent. BM3 initially bound to the DNA topoisomerase IIa enzyme, then to DNA. As a result, the tested benzothiazole derivatives were obtained as strong topoisomerase IIa inhibitors. The benzothiazole tosylated salt form BM3 was found as the most effective topoisomerase IIa inhibitor. BM3's mechanisms of action might be its direct interaction with the enzyme. BM3's minor groove-binding property might also contribute to this action. Hence, BM3 could be a good candidate as a new anticancer agent.

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Section: Introductionmentioning

confidence: 99%

Benzothiazole derivatives as human DNA topoisomerase IIα inhibitors

et al. 2013

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“…33,34 Our results also prove that novel modifications of amidinobenzimidazole molecules with the 2-pyridyl substituent at position C-2 could enrich their antiviral potentials and direct the synthetic research to novel antiviral lead molecules.…”

Section: Resultsmentioning

confidence: 58%

Synthesis, antiviral and antitumor activity of 2-substituted-5-amidino-benzimidazoles

Starčević

Kralj

Ester

et al. 2007

Bioorganic & Medicinal Chemistry

202

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We have prepared a set of heterocyclic benzimidazole derivatives bearing amidino substituents at C-5 of benzimidazole ring, by introducing various heterocyclic nuclei (pyridine, N-methyl-pyrrole or imidazole) at C-2, and evaluated their antitumor and antiviral activities. The most pronounced antiproliferative activity was shown with compounds 6 and 9, having imidazolinylamidino-substituent. Interestingly, all compounds show remarkable selectivity towards breast cancer cell line MCF-7. The most distinct and selective antiviral activity towards Coxackieviruses and Echoviruses was observed with compounds having pyridine ring at C-2. Especially interesting was fairly strong activity of 4 and 8 toward adenoviruses, which could be considered as leads against adenoviral replication.

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“…In particular, it is active against poliovirus 1-3, coxsackie B1-6 virus and A9, and echovirus 1-9, 11-21, 24-27 [82]. The 2-(4-pyridylaminomethyl)benzimidazol derivatives have one or two aromatic rings linked with a spacer much shorter than those of the WIN type compounds, probably resulting in reduced antiviral activity [82][83][84].…”

Section: Azolyalkyloxy Compoundsmentioning

confidence: 99%

The Efficacy of Viral Capsid Inhibitors in Human Enterovirus Infection and Associated Diseases

Li¹,

Wang²,

Shih³

et al. 2007

CMC

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Enteroviruses are members of picornavirus family which causes diverse and severe diseases in humans and animals. Clinical manifestations of enterovirus infections include fever, hand, foot, and mouth disease, and herpangina. Enteroviruses also cause potentially severe and life-threatening infections such as meningitis, encephalitis, myocarditis, polio-like syndrome, and neonatal sepsis. With the emergence of enterovirus all over the world as the major causative agent of HFMD fatalities in recent years and in the absence of any effective anti-enteroviral therapy, there is clearly a need to find a specific antiviral therapy. Steps such as viral attachment, uncoating, viral RNA replication, and protein synthesis in the replication cycle can serve as potential targets for antiviral agents. Agents targeted at viral protein 1 (VP1), a relatively conserved capsid structure mediating viral adsorption and uncoating process, is of great potential to be anti-enterovirus drugs. Recently, considerable efforts have been made in the development of antiviral compounds targeting the capsid protein of enterovirus. This review summarizes the development of small molecules targeting enteroviral capsid protein as effective antiviral therapy.

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Antiviral and Antiproliferative Activity in vitro of some New Benzimidazole Derivatives

Cited by 10 publications

References 15 publications

Benzothiazole derivatives as human DNA topoisomerase IIα inhibitors

Benzothiazole derivatives as human DNA topoisomerase IIα inhibitors

Synthesis, antiviral and antitumor activity of 2-substituted-5-amidino-benzimidazoles

The Efficacy of Viral Capsid Inhibitors in Human Enterovirus Infection and Associated Diseases

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