Abstract:Numerous reports have shown that conjugated benzimidazole derivatives possess various kinds of biological activities, including anticancer properties. In this report, we designed and synthesized 24 new molecules comprising a benzimidazole ring, arene, and alkyl chain-bearing cyclic moieties. The results showed that the N-substituted benzimidazole derivatives bearing an alkyl chain and a nitrogen-containing 5- or 6-membered ring enhanced the cytotoxic effects on human breast adenocarcinoma (MCF-7) and human ova… Show more
“…Hsieh et al [ 25 ] synthesized (E)-1-(1-allyl-1H-benzo[d]imidazol-2-yl)-3-(4-substituted phenyl) prop-2-en-1-one by using (Scheme 15 ) and evaluated for anticancer activity against different cell lines such as A549, MCF-7, HepG2, and OVCAR-3 by MTT assay using cisplatin as a reference drug. The conclusion of anticancer activity was presented in (Table 15 , Hsieh et al [ 25 ]). Scheme 15 Synthesis of imidazole derivatives …”
Section: Main Textmentioning
confidence: 99%
“…The conclusion of anticancer activity was presented in (Table 15 , Hsieh et al [ 25 ]). Scheme 15 Synthesis of imidazole derivatives …”
Section: Main Textmentioning
confidence: 99%
“…There are different examples of commercially available drugs which consist 1,3,4-oxadiazole ring (Table 1 ) such as clemizole (antihistaminic agent), etonitazene (analgesic), enviroxime (antiviral), irtemazole, astemizole (antihistamine), omeprazole, pantoprazole (antiulcer), thiabendazole (antihelmintic), nocodazole (antinematodal) [ 22 ], metronidazole and nitrosoimidazole (bactericidal), megazol (trypanocidal) [ 12 ], azathioprine (anti-rheumatoid arthritis), tinidazole, ornidazole (antiprotozoal and antibacterial), satranidazole (amoebiasis), cimetidine (gastric ulcer), carbimazole (against thyroid disorder), tolazoline (vasodilator action), naphazoline (vasoconstrictor), tetrahydrozoline (vasoconstrictor) [ 16 ], etomidate, lansoprazole, flumazenil, methimazole, pilocarpine [ 19 ], ketoconazole [ 23 ], dacarbazine (anticancer) [ 24 ], pimobendan (calcium sensitizer and phosphodiesterase inhibitor) [ 25 ], fenbendazole [ 26 ].…”
Imidazole is a five-membered heterocyclic moiety that possesses three carbon, two nitrogen, four hydrogen atoms, and two double bonds. It is also known as 1, 3-diazole. It contains two nitrogen atoms, in which one nitrogen bear a hydrogen atom, and the other is called pyrrole type nitrogen. The imidazole name was reported by Arthur Rudolf Hantzsch (1857â1935) in 1887. 1, 3-diazole is an amphoteric in nature i.e. it shows both acidic and basic properties. It is a white or colorless solid that is highly soluble in water and other polar solvents. Due to the presence of a positive charge on either of two nitrogen atom, it shows two equivalent tautomeric forms. Imidazole was first named glyoxaline because the first synthesis has been made by glyoxal and ammonia. It is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. The derivatives of 1, 3-diazole show different biological activities such as antibacterial, antimycobacterial, anti-inflammatory, antitumor, antidiabetic, anti-allergic, antipyretic, antiviral, antioxidant, anti-amoebic, antihelmintic, antifungal and ulcerogenic activities, etc. as reported in the literature. There are different examples of commercially available drugs in the market which contains 1, 3-diazole ring such as clemizole (antihistaminic agent), etonitazene (analgesic), enviroxime (antiviral), astemizole (antihistaminic agent), omeprazole, pantoprazole (antiulcer), thiabendazole (antihelmintic), nocodazole (antinematodal), metronidazole, nitroso-imidazole (bactericidal), megazol (trypanocidal), azathioprine (anti rheumatoid arthritis), dacarbazine (Hodgkin's disease), tinidazole, ornidazole (antiprotozoal and antibacterial), etc. This present review summarized some pharmacological activities and various kinds of synthetic routes for imidazole and their derived products.
“…Hsieh et al [ 25 ] synthesized (E)-1-(1-allyl-1H-benzo[d]imidazol-2-yl)-3-(4-substituted phenyl) prop-2-en-1-one by using (Scheme 15 ) and evaluated for anticancer activity against different cell lines such as A549, MCF-7, HepG2, and OVCAR-3 by MTT assay using cisplatin as a reference drug. The conclusion of anticancer activity was presented in (Table 15 , Hsieh et al [ 25 ]). Scheme 15 Synthesis of imidazole derivatives …”
Section: Main Textmentioning
confidence: 99%
“…The conclusion of anticancer activity was presented in (Table 15 , Hsieh et al [ 25 ]). Scheme 15 Synthesis of imidazole derivatives …”
Section: Main Textmentioning
confidence: 99%
“…There are different examples of commercially available drugs which consist 1,3,4-oxadiazole ring (Table 1 ) such as clemizole (antihistaminic agent), etonitazene (analgesic), enviroxime (antiviral), irtemazole, astemizole (antihistamine), omeprazole, pantoprazole (antiulcer), thiabendazole (antihelmintic), nocodazole (antinematodal) [ 22 ], metronidazole and nitrosoimidazole (bactericidal), megazol (trypanocidal) [ 12 ], azathioprine (anti-rheumatoid arthritis), tinidazole, ornidazole (antiprotozoal and antibacterial), satranidazole (amoebiasis), cimetidine (gastric ulcer), carbimazole (against thyroid disorder), tolazoline (vasodilator action), naphazoline (vasoconstrictor), tetrahydrozoline (vasoconstrictor) [ 16 ], etomidate, lansoprazole, flumazenil, methimazole, pilocarpine [ 19 ], ketoconazole [ 23 ], dacarbazine (anticancer) [ 24 ], pimobendan (calcium sensitizer and phosphodiesterase inhibitor) [ 25 ], fenbendazole [ 26 ].…”
Imidazole is a five-membered heterocyclic moiety that possesses three carbon, two nitrogen, four hydrogen atoms, and two double bonds. It is also known as 1, 3-diazole. It contains two nitrogen atoms, in which one nitrogen bear a hydrogen atom, and the other is called pyrrole type nitrogen. The imidazole name was reported by Arthur Rudolf Hantzsch (1857â1935) in 1887. 1, 3-diazole is an amphoteric in nature i.e. it shows both acidic and basic properties. It is a white or colorless solid that is highly soluble in water and other polar solvents. Due to the presence of a positive charge on either of two nitrogen atom, it shows two equivalent tautomeric forms. Imidazole was first named glyoxaline because the first synthesis has been made by glyoxal and ammonia. It is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. The derivatives of 1, 3-diazole show different biological activities such as antibacterial, antimycobacterial, anti-inflammatory, antitumor, antidiabetic, anti-allergic, antipyretic, antiviral, antioxidant, anti-amoebic, antihelmintic, antifungal and ulcerogenic activities, etc. as reported in the literature. There are different examples of commercially available drugs in the market which contains 1, 3-diazole ring such as clemizole (antihistaminic agent), etonitazene (analgesic), enviroxime (antiviral), astemizole (antihistaminic agent), omeprazole, pantoprazole (antiulcer), thiabendazole (antihelmintic), nocodazole (antinematodal), metronidazole, nitroso-imidazole (bactericidal), megazol (trypanocidal), azathioprine (anti rheumatoid arthritis), dacarbazine (Hodgkin's disease), tinidazole, ornidazole (antiprotozoal and antibacterial), etc. This present review summarized some pharmacological activities and various kinds of synthetic routes for imidazole and their derived products.
“…A series of benzimidazole-chalcone hybrids synthesized by Hsieh et al were screened for anticancer activity against A549, MCF-7, HepG2, and OVCAR-3 cancer cell lines [ 182 ]. Compounds 211 â 213 were active on all four cell lines tested, with IC 50 values < 15 ”M.…”
Section: Anticancer Activities Shown By Imidazole Derivatives Through Undefined Mechanismsmentioning
Nitrogen-containing heterocyclic rings are common structural components of marketed drugs. Among these heterocycles, imidazole/fused imidazole rings are present in a wide range of bioactive compounds. The unique properties of such structures, including high polarity and the ability to participate in hydrogen bonding and coordination chemistry, allow them to interact with a wide range of biomolecules, and imidazole-/fused imidazole-containing compounds are reported to have a broad spectrum of biological activities. This review summarizes recent reports of imidazole/fused imidazole derivatives as anticancer agents appearing in the peer-reviewed literature from 2018 through 2020. Such molecules have been shown to modulate various targets, including microtubules, tyrosine and serine-threonine kinases, histone deacetylases, p53-Murine Double Minute 2 (MDM2) protein, poly (ADP-ribose) polymerase (PARP), G-quadraplexes, and other targets. Imidazole-containing compounds that display anticancer activity by unknown/undefined mechanisms are also described, as well as key features of structure-activity relationships. This review is intended to provide an overview of recent advances in imidazole-based anticancer drug discovery and development, as well as inspire the design and synthesis of new anticancer molecules.
“…Due to their various biological and pharmacological properties, chalcones and its derivatives are intensely involved in the medicinal and industrial aspects [ 81 ]. Natural and synthetic chalcones exhibit a wide variety of biological properties including anti-proliferative [ 82 ], anti-inflammatory [ 83 ], anti-cancer [ 84 ], anti-tubercular and anti-bacterial [ 85 ], anti-fungal [ 86 ], anti-oxidant [ 87 ] and anti-leishmanial activities [ 88 ]. In addition, naturally occurring chalcones are precursors in the biosynthesis of chromanones and flavanones and play a significant role in the plant protection against ultraviolet radiation, diseases and insects [ 89 ].…”
Section: An Overview Of Chalcones Derivatives As Possible Therapeuticmentioning
Graphical abstract
Medicinal chemistry can rightfully be regarded as a cornerstone in the public health of our modern society that combines chemistry and pharmacology with the aim of designing and developing new pharmaceutical compounds. For this purpose, many chemical techniques as well as new computational chemistry applications are used to study the utilization of drugs and their biological effects. In the biological interface, medicinal chemistry constitutes a group of interdisciplinary sciences, as well as controlling its organic, physical and computational pillars. Therefore, medicinal chemists working to design an integrated and developing system that portends an era of novel and safe tailored drugs either by synthesizing new pharmaceuticals or to improving the processes by which existing pharmaceuticals are made. It includes researching the effects of synthetic, semi-synthetic and natural biologically active substances based on molecular interactions in terms of molecular structure with triggered functional groups or the specific physicochemical properties. The present work focuses on the literature survey of chemical diversity of phenoxy acetamide and its derivatives (Chalcone, Indole and Quinoline) in the molecular framework in order to get complete information regarding pharmacologically interesting compounds of widely different composition. From a biological and industrial point of view, this literature review may provide an opportunity for the chemists to design new derivatives of phenoxy acetamide and its derivatives that proved to be the successful agent in view of safety and efficacy to enhance life quality.
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