Synthesis and Antitumor Activity of 1,3,4-Thiadiazole Derivatives Bearing Coumarine Ring

Gomha, Sobhi M.; Abdel‐aziz, Hassan M.

doi:10.3987/com-14-13146

Cited by 59 publications

(45 citation statements)

References 24 publications

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“…It was also found that many of these derivatives might block proliferation of various cancer cell lines . In view of the findings mentioned in the preceding texts, and in continuation of our research work aimed at the synthesis of a variety of heterocyclic systems for biological and pharmacological evaluations , we report in the present work an efficient method for the synthesis of a series of new pyridine derivatives pendant to pyrazole moiety.…”

Section: Introductionmentioning

confidence: 76%

Synthetic Utility of Pyridinium Bromide: Synthesis and Antimicrobial Activity of Novel 2,4,6‐Trisubstituted Pyridines Having Pyrazole Moiety

Gomha

Dawood

2017

Journal of Heterocyclic Chem

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Fourteen potentially bioactive pyridines, pendant to pyrazole moiety, were synthesized and evaluated in vitro for their antimicrobial potential. Treatment of 2‐bromo‐1‐(5‐methyl‐1‐phenyl‐1H‐pyrazol‐4‐yl)ethanone with pyridine afforded the corresponding pyridinium bromide salt. Reaction of the latter salt with α,β‐unsaturated ketones yielded the corresponding 2,4,6‐trisubstituted pyridine derivatives. The structures of the synthesized products were confirmed by all possible spectral data. The antimicrobial activity of some selected products was evaluated by using well‐diffusion agar assay and minimum inhibitory concentration determination, and the results revealed good‐to‐moderate activities compared with reference drugs.

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Section: Introductionmentioning

confidence: 76%

Synthetic Utility of Pyridinium Bromide: Synthesis and Antimicrobial Activity of Novel 2,4,6‐Trisubstituted Pyridines Having Pyrazole Moiety

Gomha

Dawood

2017

Journal of Heterocyclic Chem

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“…The 1,2,4‐triazolopyrimidines have attracted growing interest because of their important pharmacological activities, such as antitumor potency, antimalarial, antimicrobial, anti‐inflammatory, and macrophage activation . In view of all these reports and in continuation of our previous work in synthesis of bioactive pyrazoles , herein, we are interested in synthesizing a new series of azolopyrimidines and pyrido[2,3‐ d ][1,2,4]triazolo[4,3‐ a ]pyrimidinones using pyrazolylchalcones as common precursor and evaluate these compounds for their antimicrobial activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Activity of Novel Azolopyrimidines and Pyrido‐Triazolo‐Pyrimidinones Incorporating Pyrazole Moiety

Abbas

Abdallah

Gomha

et al. 2017

Journal of Heterocyclic Chem

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A new series of azolopyrimidine derivatives incorporating pyrazole moiety were synthesized by reaction of 1‐(pyrazol‐3‐yl)‐2‐propenone with a number of heterocyclic amines in the presence of a catalytic amount of acetic acid. The mechanism of formation of the products was also discussed, and the structure assigned was elucidated based on both elemental and spectral analyses data. In addition, 7‐(pyrazolyl)‐2‐thioxo‐5‐phenyl‐1,3‐dihydropyrido[2,3‐d]pyrimidin‐4‐one was used as starting material for preparation of a new series of pyridotriazolopyrimidines via its reaction with a variety of hydrazonoyl chlorides in dioxane using triethylamines as catalyst. The assigned structure for these products was also proved via elemental analysis and spectroscopic techniques (IR, 1H NMR, and Mass). Moreover, the antimicrobial activity of some selected examples of the new products was evaluated, and the results obtained revealed high activity of compound 20a against the Gram positive bacteria Staphylococcus aureus and the Gram negative bacteria Klebsiella pneumonie. All the tested compounds have no antifungal activity.

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“…In light of the above findings and in continuation of our efforts to synthesize new anticancer compounds [43][44][45][46][47][48][49][50][51][52], the aim of presented report is to synthesize a new series of pyrazolyl-pyridines via multicomponent reactions which are expected to be active as antitumor agents.…”

Section: Introductionmentioning

confidence: 99%

An Efficient Synthesis of Novel Pyrazole-Based Heterocycles as Potential Antitumor Agents

et al. 2017

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Abstract:A new series of pyrazolylpyridines was prepared by reaction of ethyl-3-acetyl-1,5-diphenyl-1H-pyrazole-4-carboxylate with the appropriate aldehyde, malononitrile, or ethyl acetoacetate and an excess of ammonium acetate under reflux in acetic acid. Similarly, two novel bipyridine derivatives were prepared by the above reaction using terephthaldehyde in lieu of benzaldehyde derivatives. In addition, a series of 1,2,4-triazolo[4,3-a]pyrimidines was synthesized by a reaction of 6-(pyrazol-3-yl)pyrimidine-2-thione with a number of hydrazonoyl chlorides in dioxane and in the presence of triethylamine. The structure of the produced compounds was established by elemental analyses and spectral methods, and the mechanisms of their formation was discussed. Furthermore, the pyrazolyl-pyridine derivatives were tested as anticancer agents and the results obtained showed that some of them revealed high activity against human hepatocellular carcinoma (HEPG2) cell lines.

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Synthesis and Antitumor Activity of 1,3,4-Thiadiazole Derivatives Bearing Coumarine Ring

Cited by 59 publications

References 24 publications

Synthetic Utility of Pyridinium Bromide: Synthesis and Antimicrobial Activity of Novel 2,4,6‐Trisubstituted Pyridines Having Pyrazole Moiety

Synthetic Utility of Pyridinium Bromide: Synthesis and Antimicrobial Activity of Novel 2,4,6‐Trisubstituted Pyridines Having Pyrazole Moiety

Synthesis and Antimicrobial Activity of Novel Azolopyrimidines and Pyrido‐Triazolo‐Pyrimidinones Incorporating Pyrazole Moiety

An Efficient Synthesis of Novel Pyrazole-Based Heterocycles as Potential Antitumor Agents

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