Benzimidazole derivatives as potent and isoform selective tumor-associated carbonic anhydrase IX/XII inhibitors

Uslu, Azize Gizem; Maz, Tuğçe Gür; Nocentini, Alessio; Banoğlu, Erden; Çalışkan, Burcu

doi:10.1016/j.bioorg.2019.103544

Cited by 18 publications

(17 citation statements)

References 30 publications

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“…[ 10,59 ] The binding pattern of butyrylcholine to the active site of butyrylcholinesterase (BChE) (pdb: 1p0i) (b). [ 59,60 ] The estimated binding model of compound 2d to the active site of AChE (c). The estimated binding model of compound 2d to the active site of BChE (d)…”

Section: Resultsmentioning

confidence: 99%

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Synthesis, characterization, and biological evaluation of some novel Schiff bases as potential metabolic enzyme inhibitors

Çakmak

Başaran

Şentürk

2022

Archiv der Pharmazie

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In this study, a series of novel Schiff base derivatives containing a pyrazolone ring (2a-e) were designed, successfully synthesized for the first time, and characterized by elemental analysis and some spectroscopic methods. These compounds were tested for their inhibitory activities on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and the human carbonic anhydrase isoenzymes I and II (hCA I and II). All synthesized molecules indicated significant inhibition effects with IC 50 values ranging from 14.15 to 107.62 nM against these enzymes. Compound 2d showed the most potent inhibitory activity among the tested molecules toward AChE and BChE (IC 50 = 15.07 and 14.15 nM) compared to the standard drug neostigmine. We determined that the IC 50 values of the tested molecules ranged between 16.86 and 57.96 nM for hCA I and 15.24-46.21 nM for hCA II. As a consequence, we may say that some of the Schiff base derivatives may be used as potential drug candidates in later studies.

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Section: Resultsmentioning

confidence: 99%

“…[10,59] The binding pattern of butyrylcholine to the active site of butyrylcholinesterase (BChE) (pdb: 1p0i) (b). [59,60] The estimated binding model of compound The InChI codes of the investigated compounds are provided as Supporting Information.…”

Section: Biochemical Studiesmentioning

confidence: 99%

Synthesis, characterization, and biological evaluation of some novel Schiff bases as potential metabolic enzyme inhibitors

Çakmak

Başaran

Şentürk

2022

Archiv der Pharmazie

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“…Zubrien and coworkers synthesized and report sulfonyl anchored with benzene or benzimidazole rings 79 (a–f), and these derivatives act as inhibitors of carbonic anhydrases. Carbonic anhydrases are ubiquitous metalloenzymes, which catalyze the reversible hydration reaction of CO 2 into protons and bicarbonate [ 53 , 54 ]. Among these compounds, 79b showed the best inhibitors activities on CA I, II, VII, and XIII exhibiting affinities ( Figure 9 ) [ 53 , 54 ].…”

Section: Bioactivities Of Benzimidazole-sulfonyl Scaffolds and Their ...mentioning

confidence: 99%

Synthesis of Benzimidazole-Sulfonyl Derivatives and Their Biological Activities

Mulugeta

Samuel

2022

Biochemistry Research International

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Currently, the synthesis of new compounds with potential bioactivities has become a central issue in the drug discovery arena. Among these new compounds, benzimidazole-sulfonyl scaffolds have vital applications in the fields of pharmaceuticals industries. Benzimidazole and sulfonyl compounds have remarkable biological activities, such as antibacterial, antifungal, anti-inflammatory, antiproliferative, carbonic anhydrase inhibitory, and α-amylase inhibitory activities. Furthermore, recent literature mentions the synthesis and bioactivities of some benzimidazole-sulfonyl hybrids. In this review, we focus on reviewing the synthesis of these hybrid scaffolds and their various types of biological activities of the compounds.

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“…Uslu et al [69] prepared a series of 2-arylbenzimidazole derivatives containing sulfonamide functionality as well as carboxylic acid, hydroxamic acid, carboxamide and boronic acid functionalities, which act as human CA inhibitors. The sulfonamide containing benzimidazole compound 4 derivatives (fig.…”

Section: Human Carbonic Anhydrase Ix/xii Inhibitorsmentioning

confidence: 99%

Pyridine Moiety: Recent Advances in Cancer Treatment

Sahu¹,

Mishra²,

Kumar³

et al. 2021

ijps

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Pyridine is an imperative pharmacophore, a privileged scaffold and an exceptional heterocyclic system in the field of drug discovery which provides many opportunities in study/explore this moiety as an anticancer agent by acting on various receptors of utmost importance. Several pyridine derivatives are reported to inhibit tubulin polymerization, androgen receptors, human carbonic anhydrase, kinase, topoisomerase enzyme and many other targets for controlling and curing global health issue of cancer. Now a days in combination with other moieties researchers are focusing for development of pyridine new entities for the treatment of cancer. This review throws light on recent biological expansions of pyridine along with their structure activity relationships/molecular docking to deliver association between various synthesized newer derivatives and receptor sites.

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Benzimidazole derivatives as potent and isoform selective tumor-associated carbonic anhydrase IX/XII inhibitors

Cited by 18 publications

References 30 publications

Synthesis, characterization, and biological evaluation of some novel Schiff bases as potential metabolic enzyme inhibitors

Synthesis, characterization, and biological evaluation of some novel Schiff bases as potential metabolic enzyme inhibitors

Synthesis of Benzimidazole-Sulfonyl Derivatives and Their Biological Activities

Pyridine Moiety: Recent Advances in Cancer Treatment

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