The identification of potent and selective imidazole-based inhibitors of B-Raf kinase

Takle, Andrew K.; Brown, Murray J. B.; Davies, Susannah; Dean, David K.; Francis, Gerraint; Gaiba, Alessandra; Hird, Alex; King, Frank D.; Lovell, Peter J.; Naylor, A.; Reith, Alastair D.; Steadman, Jon G.A.; Wilson, David M.

doi:10.1016/j.bmcl.2005.09.072

Cited by 184 publications

(81 citation statements)

References 9 publications

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“…Different substituted imidazoles show variable biological activities such as antibacterial, anti-allergic, anti-inflammatory, antitumor analgesic, glucagon receptor antagonism therapeutic agents, and pesticides [6][7][8][9] . Also, some of them are known as inhibitors of P38 MAP 10 kinase and B Raf kinase 11 . Recent advances in green chemistry and organometallic catalysis has extended the application of imidazoles as ionic liquids [12][13][14] and N-heterocyclic carbenes 15 .…”

Section: Oriental Journal Of Chemistrymentioning

confidence: 99%

Solvent-Free Synthesis of 1,2,4,5-Tetrasubstituted Imidazoles Using Nano Fe3O4@SiO2-OSO3H as a Stable and Magnetically Recyclable Heterogeneous Catalyst

Yadegarian¹,

Davoodnia²,

Nakhaei³

2015

Orient. J. Chem

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Nano-Fe 3 O 4 encapsulated-silica particles bearing sulfonic acid groups (Fe 3 O 4 @SiO 2 -OSO 3 H) has been used as an efficient and magnetically separable heterogeneous catalyst for the synthesis of 1,2,4,5-tetrasubstituted imidazoles by one-pot, four-component reaction of benzil, aromatic aldehydes, primary amines, and ammonium acetate under neat conditions. The effect of various reaction parameters, such as reaction temperature, catalyst loading and solvent effect, were studied. The desired products are obtained in relatively short reaction times with high yields. Importantly, the catalyst could be easily separated from the reaction mixture by a permanent magnet and reused for several times without the significant loss of its activity.

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Section: Oriental Journal Of Chemistrymentioning

confidence: 99%

Solvent-Free Synthesis of 1,2,4,5-Tetrasubstituted Imidazoles Using Nano Fe3O4@SiO2-OSO3H as a Stable and Magnetically Recyclable Heterogeneous Catalyst

Yadegarian¹,

Davoodnia²,

Nakhaei³

2015

Orient. J. Chem

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“…Imidazole and its analogues are centre of attraction for researchers around the globe due to their diverse bioactivities. Imidazole derivatives were reported to be involved in the biosynthesis of interleukin-1 (IL-1) 2 and were also reported to function as cyclooxygenase-2 (COX-2) [3] B-Raf kinase 4 , transforming growth factor b1 (TGF-b1) type 1 activin receptor-like kinase (ALk5) 5 and p38 MAP kinase 6 inhibitors. Appropriately substituted imidazoles were used as CB1 cannabinoid receptor antagonists 7 , modulators of P-glycoprotein (P-gp) mediated multidrug resistance (MDR) 8 and glucagon receptors 9 .…”

Section: Introductionmentioning

confidence: 99%

“…Condensation involving cyclodehydration of different aldehyde/substituted aldehydes, anilines/substituted anilines with benzil is an important and mostly employed method for tetrasubstituted imidazole formation in organic synthesis. The various types of bulk catalysts, such as DABCO 21 , HClO 4 The recovery of the catalyst and separation of product is easier in case of solvent free reactions than conventional routes. Use of nanoparticles as catalysts in organic transformations is one of the emerging trends currently.…”

Section: Introductionmentioning

confidence: 99%

An Efficient, Solvent Free One Pot Synthesis of Tetra substitue dimidazoles Catalyzed by Nanocrystalline γ-alumina

Shelke¹,

Rajbhoj²,

Nimase³

et al. 2016

Orient. J. Chem

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γ-Alumina nanoparticles (γ-Al 2 O 3 NPs) have been successfully synthesized by electrochemical reduction method. The aqueous solution of tetrapropylammonium bromide was used as an electrolyte cum stabilizer. To prevent spontaneous agglomeration and control nanoparticles size various parameter such as current density, distance between electrodes and concentrations of electrolyte are optimized. γ-Al 2 O 3 NPs thus synthesized were characterized by sophisticated analytical techniques including X-ray diffraction, scanning electron microscopy, energy dispersive spectrophotometer and high-resolution transmission electron microscopy These synthesized γ-Al 2 O 3 NPs were tested used as a catalyst for one pot synthesis of tetraaryl imidazole derivatives from the cyclodehydration and condensation of benzil, aromatic aldehyde, anilines and ammonium acetate under solvent free condition. This method has various advantages like convenient work-up procedure, environmentally benign and less reaction times along with excellent yields. Easy availability, several times recyclability, very simple isolation and eco-friendliness were some attractive features of the nanocrystalline γ-Al 2 O 3 catalyst.

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“…[3] Various derivatives of imidazoles are used as anti-bacterial, [4] anti-tumoral, [5] anti-inflammatory, [6] fungicidal, antimycotic, anti-ulcerative, antibiotic and analgesic [7] agents, herbicides and plant growth regulators. [2] Additionally, they are also used as inhibitors of p38 MAP kinases, [8] B-Raf kinases, cyclooxygenase-2, transforming growth factor b1, type-1 activin receptor-like kinase, [9][10][11] in IL-1 biosynthesis, [12] as therapeutic agents, glucagon receptors, [13] heme oxygenase-1 inhibitors, heme oxygenase inhibitors, fatty acid amide hydrolase inhibitors [14] and as photosensitive compounds in photography. [15] Further, they are also found as a core structural skeleton in many important biological compounds like histidine, histamine and biotin and in other drug moieties like trifenagrel, eprosartan and losartan.…”

Section: Introductionmentioning

confidence: 99%

Co(II) anchored glutaraldehyde crosslinked magnetic chitosan nanoparticles (MCS) for synthesis of 2,4,5‐trisubstituted and 1,2,4,5‐tetrasubstituted imidazoles

Singh

Rajput

2017

Applied Organom Chemis

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A simple, highly efficient and green synthesis of 2,4,5-trisubsituted and 1,2,4,5-tetrasubstituted imidazoles was developed using a novel MCS-GT@Co(II) magnetically recoverable and recyclable catalyst under refluxing conditions with ethanol as a solvent. The catalyst was prepared by immobilization of chitosan onto Fe 3 O 4 using glutaraldehyde as crosslinker followed by Co(II) ion immobilization via cobalt acetate. The catalyst was characterized using various techniques. For organic products determination, 1 H NMR, 13 C NMR and Fourier transform infrared spectroscopies were used. The reaction was also tried with individual components of the catalyst, but the synergistic effect of the components in the prepared catalyst showed the highest yield and shortest reaction time.

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The identification of potent and selective imidazole-based inhibitors of B-Raf kinase

Cited by 184 publications

References 9 publications

Solvent-Free Synthesis of 1,2,4,5-Tetrasubstituted Imidazoles Using Nano Fe3O4@SiO2-OSO3H as a Stable and Magnetically Recyclable Heterogeneous Catalyst

Solvent-Free Synthesis of 1,2,4,5-Tetrasubstituted Imidazoles Using Nano Fe3O4@SiO2-OSO3H as a Stable and Magnetically Recyclable Heterogeneous Catalyst

An Efficient, Solvent Free One Pot Synthesis of Tetra substitue dimidazoles Catalyzed by Nanocrystalline γ-alumina

Co(II) anchored glutaraldehyde crosslinked magnetic chitosan nanoparticles (MCS) for synthesis of 2,4,5‐trisubstituted and 1,2,4,5‐tetrasubstituted imidazoles

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