Solvent-free synthesis and anticancer activity evaluation of benzimidazole and perimidine derivatives

Kumar, Anuj; Banerjee, Somesh; Roy, Partha; Sondhi, Sham M.; Sharma, Anuj

doi:10.1007/s11030-017-9790-3

Cited by 22 publications

(16 citation statements)

References 34 publications

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“…Triazole containing 4,5,6,7-tetrabromo-1 H -benzimidazole derivatives 258–259 bearing carboxyl substituent manifested the most prominent inhibitory effect against protein kinase 2 (CK2) with binding affinity value in the range of 1.96–0.91 µM ( Chojnacki et al, 2017 ). Compounds 260–264 exerted antiproliferative property in MTT assay against five human cancer cell lines, breast (T47D), lung (NCl H-522), liver (HepG2), colon (HCT-15) and ovary (PA-1) with IC 50 (mean ± SD) value of 7.5 ± 0.3 to 14.6 ± 0.4 μM ( Kumar et al, 2018 ). Upon assessment of antiproliferative property against four cancer cell lines (HeLa, MCF-7, A549 and DU-145 alongside normal HEK-293 cell line), Baig et al ( Baig et al, 2018 ) enumerated noteworthy IC 50 (1.08 µM) of derivative 265 against A549 cell line.…”

Section: Biological Activitiesmentioning

confidence: 99%

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

et al. 2021

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Nowadays, nitrogenous heterocyclic molecules have attracted a great deal of interest among medicinal chemists. Among these potential heterocyclic drugs, benzimidazole scaffolds are considerably prevalent. Due to their isostructural pharmacophore of naturally occurring active biomolecules, benzimidazole derivatives have significant importance as chemotherapeutic agents in diverse clinical conditions. Researchers have synthesized plenty of benzimidazole derivatives in the last decades, amidst a large share of these compounds exerted excellent bioactivity against many ailments with outstanding bioavailability, safety, and stability profiles. In this comprehensive review, we have summarized the bioactivity of the benzimidazole derivatives reported in recent literature (2012–2021) with their available structure-activity relationship. Compounds bearing benzimidazole nucleus possess broad-spectrum pharmacological properties ranging from common antibacterial effects to the world’s most virulent diseases. Several promising therapeutic candidates are undergoing human trials, and some of these are going to be approved for clinical use. However, notable challenges, such as drug resistance, costly and tedious synthetic methods, little structural information of receptors, lack of advanced software, and so on, are still viable to be overcome for further research.

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Section: Biological Activitiesmentioning

confidence: 99%

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

et al. 2021

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“…A. Kumar et al [63] synthesized an array of 1 H ‐benzimidazole tetracyclic derivatives by microwave irradiation method. The synthesized compounds were screened for their antiproliferative activities against T47D (breast), NCl H‐522 (lung), HCT‐15 (colon), PA‐1 (ovary), and Hep G2 (liver) human cancer cell lines by MTT assay.…”

Section: Benzimidazole As Target Oriented Anticancer Agentsmentioning

confidence: 99%

Benzimidazole based derivatives as anticancer agents: Structure activity relationship analysis for various targets

Satija

Sharma

Madan

et al. 2021

Journal of Heterocyclic Chem

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Benzimidazole, the benzo derivative of imidazole, is a class of bicyclic aromatic organic compound consisting of six‐membered benzene ring fused to five‐membered imidazole at 4‐ and 5‐positions of the imidazole ring. It is a vital pharmacophore of many biologically active heterocyclic compounds with a variety of pharmacological activities. Over the time, benzimidazole and its derivatives have evolved as vibrant heterocyclic systems due to their potency in a wide range of bioactive compounds like analgesics, antifungals, anti‐inflammatory, antihypertensives, proton pump inhibitors, anti‐HIV, antiviral, and so on. Multi‐drug resistance in cancer that led to the failure of many chemotherapeutic drugs is a major concern. Various approaches are being developed to overcome this problem. One of them is target based drug discovery, which is an effective method to develop a novel anticancer drug. To develop newer drugs, previously reported work needs to be studied. Keeping this in mind, last 5 years literature on benzimidazole used as anticancer agents has been reviewed and summarized in the paper herein. This review article along with the target of cancer also deal with structure activity relationship of various compounds having benzimidazole ring.

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“…Among all the tested compounds, 15a, 15b, and 16 revealed high antimicrobial activity against standard drugs (Scheme 14). Kumar et al [135] designed tetracyclic and pentacyclic perimidines from NDA and dicarbonyl compounds using microwave techniques and further evaluated their ability to suppress the growth of cancer cell lines. The in vitro antiproliferative activity was studied against five human cancer cell lines (breast T47D, lung NCl H-522, liver HepG2, colon HCT-15, ovary PA-1) using the MTT assay at 10 μM concentration.…”

Section: Biologic Applicationsmentioning

confidence: 99%

Recent Advances in the Synthesis of Perimidines and their Applications

Sahiba¹,

Agarwal²

2020

Top Curr Chem (Z)

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Perimidines are versatile scaffolds and a fascinating class of N-heterocycles that have evolved significantly in recent years due to their immense applications in life sciences, medical sciences, and industrial chemistry. Their ability of molecular interaction with different proteins, complex formation with metals, and distinct behavior in various ranges of light makes them more appealing and challenging for future scientists. Various novel technologies have been developed for the selective synthesis of perimidines and their conjugated derivatives. These methods extend to the preparation of different bioactive and industrially applicable molecules. This review aims to present the most recent advancements in perimidine synthesis under varied conditions like MW radiation, ultrasound, and grinding using different catalysts such as ionic liquids, acid, metal, and nanocatalyst and also under green environments like catalyst and solvent-free synthesis. The applications of perimidine derivatives in drug discovery, polymer chemistry, photo sensors, dye industries, and catalytic activity in organic synthesis are discussed in this survey. This article is expected to be a systematic, authoritative, and critical review on the chemistry of perimidines that compiles most of the state-of-art innovation in this area.

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Solvent-free synthesis and anticancer activity evaluation of benzimidazole and perimidine derivatives

Cited by 22 publications

References 34 publications

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

Benzimidazole based derivatives as anticancer agents: Structure activity relationship analysis for various targets

Recent Advances in the Synthesis of Perimidines and their Applications

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