Synthesis and Biological Evaluation of the Pyrazole Class of Cyclooxygenase- 2-Inhibitors

Rida, S. M.; Saudi, M. N. S.; Youssef, A.-B.M.; Halim, Madiha A.

doi:10.2174/157017809788489909

Cited by 20 publications

(7 citation statements)

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“…5 , 6 . The key starting materials 1,3-diphenyl-1 H -pyrazole-4-carbaldehyde 9 [ 32 ] , 1-phenyl-3-p -tolyl-1 H -pyrazole-4-carbaldehyde 10 [ 32 ] , 3-(4-chlorophenyl)-1-phenyl-1 Hpyrazole-4-carbaldehyde 11 [ 32 ] , 3-(4-bromophenyl)-1-phenyl-1 H -pyrazole-4-carbaldehyde 12 [ 32 ] , 1-(4-nitrophenyl)-3-phenyl-1 H -pyrazole-4-carbaldehyde 13 [ 33 ] , 1-(4-nitrophenyl)-3-ptolyl-1 H -pyrazole-4-carbaldehyde 14 , 3-(4-chloro phenyl)-1-(4- nitrophenyl)-1 H -pyrazole-4-carbaldehyde 15 [ 34 ] , and 3-(4-bromophenyl)-1-(4-nitrophenyl)-1 H -pyrazole-4-carbaldehyde 16 [ 22 ] were prepared from the reaction of acetophenone or 4-substituted acetophenones with phenyl hydrazine or 4-nitrophenyl hydrazine to produce the corresponding hydrazones 1-8 , followed by Vilsmeier-Haack reaction [ 35 ] .…”

Section: Results and Discussion ▼ Chemistrymentioning

confidence: 99%

Design, Synthesis and Evaluation of Novel Benzimidazoles, Benzothiazoles and Benzofurans Incorporating Pyrazole Moiety as Antiangiogenic Agents

Rida

Youssef

Badr

et al. 2012

Arzneimittelforschung

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Novel benzimidazoles, benzothiazoles and benzofurans incorporating pyrazole moiety have been synthesized and screened for their antiangogenic activities, by testing their ability to inhibit human umbilical vein endothelial cell (HUVEC) proliferation, cord formation and migration in response to chemoattractant. 3 compounds 19, 23 and 26 showed antiangiogenic activities at non-cytotoxic concentrations. Compound 19 was the most active with chemotaxis activity data nearly comparable to that of the positive control, TNP-470. Compound 42 showed a significant cytotoxic effect on the tested cancer cell lines and less antiangiogenesis activity compared to compounds 19, 23 and 26. All the tested compounds, in contrary to TNP-470, interfered with the migratory function of HUVECs in response to vascular endothelial growth factor rather than the endothelial cells proliferation or cord formation. Moreover, a docked pose of compounds 19 and 26 was obtained bound to kinase insert domain receptor using Molecular Operating Environment module.

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Section: Results and Discussion ▼ Chemistrymentioning

confidence: 99%

Design, Synthesis and Evaluation of Novel Benzimidazoles, Benzothiazoles and Benzofurans Incorporating Pyrazole Moiety as Antiangiogenic Agents

Rida

Youssef

Badr

et al. 2012

Arzneimittelforschung

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“…The solid separated was triturated with water, fil- tered and recrystallized from methanol. Yield 91%; off white solid; M. p. 165-167 O C; FTIR (KBr, ν/cm -1 ): 3250 (NH), 2239, 2222 (2CN), 1797, 1735 (2C=O), 1610 (aromatic C=C); 1 H NMR (500 MHz, DMSO-d 6 ) δ 11.81 (s, 1H, NH), 7.97 (dd, J = 7.5 Hz, 2H), 7.88 (t, J = 7.5 Hz, 2H), 3.93 (s, 2H, CH 2 ); 13…”

Section: Synthesis 3-(cyanomethyl)-5-(13-dioxoisoindolin-2-yl)-1h-pymentioning

confidence: 99%

“…Yield 79%; yellow solid; M.p. 186-188 O C; FTIR (KBr, ν/cm -1 ): 3309 (OH), 3246 (NH), 2960 (C-H), 2227 (CN), 1737, 1708 (2C=O), 1612 (aromatic C=C); 1 H NMR (500 MHz, DMSO-d 6 ) δ 12.50 (s, 1H, NH), 9.34 (s, 1H, OH), 7.98 (s, 1H, =CH), 7.97 (dd, J = 7.7 Hz, 2H)7.84 (t, J = 7.7 Hz, 2H), 7.63 (d, J = 7.5 Hz, 2H), 6.78 (d, J = 7.5 Hz, 2H); 13…”

Section: -(1-cyano-2-(4-hydroxyphenyl)vinyl)-5-(13dioxoisoindolin-2mentioning

confidence: 99%

Design, Synthesis and Biological Estimation of Innovative Pyrazoles as Anticancer Agents Targeting Cdk2

Ibrahim¹,

Radini²,

Khidre³

2019

Acta Poloniae Pharmaceutica - Drug Research

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CDK2, which exhibits an indispensable role as an organizer of cell growth, is the powerfully studied protein Kinases objective of anticancer suppressors. The present study was dedicated to design (pharmacophore, docking, and binding energy) and to prepare an inspired derivatives of pyrazole and pyrazolo[1,5d]pyrimidine as promising anticancer agents, which can act by targeting CDK2. The promising compounds were selected according to their fit-value and binding energy scores. The anticancer activity against MCF-7 was tested for the prepared compounds and compounds 2, 3b, and 7b showed expressive activity with IC 50 1.75, 0.89 and 1.32 µM respectively. The CDK2 evaluation was carried out to estimate the efficiency of the prepared compounds as promising inhibitors. The results revealed that compound 3b with effective inhibitory activity against tumor growth and with its potent inhibition against the CDK2 enzyme with percent inhibition 86 would be a prospective anticancer agent. The prepared compounds with high biological activity could be used as lead inhibitors for the CDK2 kinase domain.

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“…It is known that sulfathiazole derivatives have a decisive new and differentiating application in various areas of chemistry. [1][2][3] The pyrazole skeleton is a common core in many pharmaceutically active compounds and is important for a wide range of pharmacological activities including anti-inflammatory, 4,5 antiviral, 6 antimicrobial, 7 antifungal, 8,9 hypoglycemic, 10,11 antihyperlipidemic, 12 cyclooxygenase-2 inhibitors, 13 CDK2/cyclinA inhibitors, 14,15 and anti-angiogenic activity. 16 Furthermore, carbonyl cyanide-phenylhydrazone is an efficient decoupler of oxidative phosphorylation sites in a mitochondrial organism.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Evaluation of Some New Pyrazolo[1,5-a]pyrimidine and Pyrazolo[1,5-c]triazine Derivatives Containing Sulfathiazole Moiety

El‐Sayed¹,

Fadda²,

El-Saadaney³

2020

ACSi

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A number of important fused heterocyclic systems have been prepared by the reaction of 4-((3,5-diamino-1H-pyrazol-4-yl)-diazenyl)-N-(thiazol-2-yl)-benzenesulfonamide with some bifunctional nucleophiles such as ethyl acetoacetate, acetylacetone or arylidenemalonononitrile derivatives to obtain pyrazolo[1,5-a]pyrimidine derivatives. The structures of the newly synthesized compounds were determined based on their IR, 1H and 13C NMR and mass spectroscopic data. Most of the compounds produced showed good antibacterial and antifungal activity

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Synthesis and Biological Evaluation of the Pyrazole Class of Cyclooxygenase- 2-Inhibitors

Cited by 20 publications

References 0 publications

Design, Synthesis and Evaluation of Novel Benzimidazoles, Benzothiazoles and Benzofurans Incorporating Pyrazole Moiety as Antiangiogenic Agents

Design, Synthesis and Evaluation of Novel Benzimidazoles, Benzothiazoles and Benzofurans Incorporating Pyrazole Moiety as Antiangiogenic Agents

Design, Synthesis and Biological Estimation of Innovative Pyrazoles as Anticancer Agents Targeting Cdk2

Synthesis and Antimicrobial Evaluation of Some New Pyrazolo[1,5-a]pyrimidine and Pyrazolo[1,5-c]triazine Derivatives Containing Sulfathiazole Moiety

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