A step-by-step synthesis of triazole-benzimidazole-chalcone hybrids: Anticancer activity in human cells+

Djemoui, Amar; Naouri, Abdelkader; Ouahrani, M. R.; Djemoui, D.; Souli, L.; Lahrech, Mokhtar; Boukenna, Leila; Albuquerque, Hélio M. T.; Saher, Liza; Rocha, Djenisa H. A.; Monteiro, Fátima Liliana; Helguero, Luísa A.; Bachari, Khaldoun; Talhi, Oualid; Silva, Artur M. S.

doi:10.1016/j.molstruc.2019.127487

Cited by 70 publications

(42 citation statements)

References 44 publications

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“…Recently, Djemoui et al ( Djemoui et al, 2020 ) synthesized several triazole-benzimidazole-chalcone hybrid compounds 271–274 and narrated potential anti-proliferative property of these derivatives against two breast cancer (T47-D and MDA-MB-231) and one prostate cancer cell line (PC3) compared to standard Doxorubicin. It is mentionable here that the chloro substituent 274 at the chalcone ring proliferated the anticancer effects.…”

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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“…The compound 42 exerted high potency than 5‐fluorouracil against cell lines such as HepG‐2, SK‐N‐SH, and MGC‐803 with IC 50 value 3.84 μM, 8.68 μM, and 2.99 μM respectively. SAR studies demonstrated that the replacement of 3,4,5‐trimethoxy with chloro led to a decline in the antiproliferative activity [58] . The compound 43 exhibited good anticancer activity against gastric cancer cell line (MGC‐803; IC 50 : 5.39 μM) and excellent activity against HepG‐2 (IC 50 : 0.53 μM) cancer cell (Figure 14).…”

Section: Imidazole Hybridizes With Other Anticancer Pharmacophoresmentioning

confidence: 99%

Hybridization of Imidazole with Various Heterocycles in Targeting Cancer: A Decade's Work

Teli¹,

Chawla²

2021

ChemistrySelect

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Cancer is the world‘s biggest global health concern. The prevalence and mortality rates of cancer remain high despite significant progress in cancer therapy. The search for more effective, as well as less toxic treatment methods for cancer, is at the focus of current studies. Approximately 24.6 million people are suffering from cancer across the world as per the world health organization (WHO). In the year 2020, approximately 10 million deaths were reported due to cancer which has emerged as the second leading cause of mortality across the globe. Anticancer medicines have played a pivotal role in the medication of different types of cancers; however, they are associated with several side effects and relevance of drug resistance which evoke an immediate need for designing of new anticancer agents with multitargeted effect. Imidazole is a heterocyclic compound privileged with considerable anticancer activities and some imidazole derivatives have already got approval to treat cancer. Many hybrid molecules are available that play an important role in the treatment of cancer like chalcone, pyrazole, purine, triazine etc., and their pharmacophore provide the anticancer drug with low drug resistance and high efficacy, with low chances of toxicity and side effects. This review provides various approaches for the drug development of new safe and efficient antitumor agents imidazole hybrids with other heterocyclic moieties. An attempt has been made to advancement of the anticancer potential of the derivatives and hybrids of imidazole having intact or condensed imidazole moiety in the last decade along with the structure‐activity relationship studies, and mechanism of action.

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“…FT-IR and DFT studies suggested that inhibitors strongly interacted as adsorbed on the metallic surface. Besides these reports, numerous plant extracts containing indole based alkaloids have been effectively tested as corrosion inhibitors for metals and alloys in various electrolytic environments [97][98][99][100][101][102][103].…”

Section: Indole Based Alkaloids As Corrosion Inhibitorsmentioning

confidence: 99%

Alkaloids as green and environmental benign corrosion inhibitors: An overview

2019

Int. J. Corros. Scale Inhib.

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Alkaloids are naturally occurring nitrogen containing organic bases that possess diverse and significant physiological effects on animals and humans. They are mostly derived from the plants. Because of their natural and biological origin, they (alkaloids) are considered as environmental benign alternatives to be used as corrosion inhibitors at the place of traditional and toxic synthetic corrosion inhibitors. Numerous alkaloids have been employed as effective corrosion inhibitors for metals and alloys in different electrolytic media. It has been established that alkaloid molecules are associated with extensive conjugation in the form of non-bonding and π-elections through which they can interact strongly and inhibit corrosion efficiently. Present review article features the collection of reports published on the topic alkaloids as corrosion inhibitors. In this review article, we also described the corrosion and its adverse effect, mechanism of corrosion and corrosion inhibition by organic corrosion inhibitors (including alkaloids) and factors affecting the inhibition property of corrosion inhibitors. Literature study suggests that most of the alkaloids are soluble in the polar electrolytic media and thereby behave as good corrosion inhibitors. Present review article describes the inhibition effect of several classes of alkaloids such as pyridine, purine and indole derivatives that have been used previously. Chemical structures alkaloids and their mode of adsorption and interactions with the metallic surface, nature of metal and electrolyte and related salient features have also been tabulated in the review.

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A step-by-step synthesis of triazole-benzimidazole-chalcone hybrids: Anticancer activity in human cells+

Cited by 70 publications

References 44 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

Hybridization of Imidazole with Various Heterocycles in Targeting Cancer: A Decade's Work

Alkaloids as green and environmental benign corrosion inhibitors: An overview

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