Morpholin-4-ium [5-cyano-6-(4-methylphenyl)-4-(morpholin-4-yl)pyrimidin-2-yl](phenylsulfonyl)amide

Mohamed-Ezzat, Reham A.; Kariuki, Benson M.; Azzam, Rasha A.

doi:10.1107/s2414314622010331

Cited by 3 publications

(1 citation statement)

References 15 publications

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“…We have lately reported diverse synthetic methods for the preparation of heterocycles using cyanohydrazones [31][32][33]. Several derivatives of these ring structures are considered significant as antimetabolites in most biochemical reactions [34][35][36].…”

Section: Introductionmentioning

confidence: 99%

Unexpected Products of the Reaction of Cyanoacetylhydrazones of Aryl/heteryl Ketones with Hydrazine: A New Route to Aryl/Heteryl Hydrazones, X-ray Structure, and In vitro Anti-proliferative Activity Against NCI 60-cell Line Panel

2023

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A new unexpected synthetic non-catalytic method for the synthesis of novel heteryl hydrazones for basemodification of nucleoside analogs has been developed. Characterizations of the products have been performed using NMR spectroscopy and single crystal x-ray diffraction analysis. Further in vitro anti-proliferative potency of the compounds against NCI 60 cell lines has been estimated. The results indicate anti-cancer activity by the compounds against several of the cancer cell lines.

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Section: Introductionmentioning

confidence: 99%

Unexpected Products of the Reaction of Cyanoacetylhydrazones of Aryl/heteryl Ketones with Hydrazine: A New Route to Aryl/Heteryl Hydrazones, X-ray Structure, and In vitro Anti-proliferative Activity Against NCI 60-cell Line Panel

2023

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Discovery of Promising Sulfadiazine Derivatives With Anti‐Proliferative Activity Against Tumor Cell Lines

Mohamed‐Ezzat,

Kariuki,

Azzam

2024

Journal of Heterocyclic Chem

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A novel series of pyrimidine sulfonamide derivatives was synthesized through a strategic approach involving the creation of substituted dihydropyrimidinyl‐benzenesulfonamides and subsequent transformation into their chlorinated analogues. These compounds were then subjected to reactions with various amines and phenols, yielding unique substituted sulfapyrimidines. These novel structures integrated essential pharmacophores such as phenols, secondary amines, and benzenesulfonamide moieties, each contributing distinct biological potencies, chemical reactivity, and enhanced pharmacological features. In the pursuit of effective anticancer agents, the newly substituted pyrimidine sulfonamides were characterized using spectroscopic and x‐ray diffraction techniques. The compounds were evaluated for their anti‐proliferative potency against the NCI 60‐cell lines panel, revealing that compound 7c exhibited significant growth inhibition across multiple cancer cell lines. Further assessment through MTT assay on HCT‐116 and MCF‐7 cell lines demonstrated cytotoxicity, while cell cycle analysis of MCF‐7 cells treated with compound 7c revealed arrest at the S phase. Moreover, the effect of 7c on programmed cell death was evaluated using the Annexin V/PI apoptosis assay. The observed promising activity positions these pyrimidine‐based scaffolds as potential candidates for future drug development, offering valuable insights for medicinal chemists engaged in the design and synthesis of anticancer drugs.

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Novel synthesis of the first new class of triazine sulfonamide thioglycosides and the evaluation of their anti-tumor and anti-viral activities against human coronavirus

Mohamed-Ezzat,

Elgemeie

2024

Nucleosides, Nucleotides & Nucleic Acids

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Morpholin-4-ium [5-cyano-6-(4-methylphenyl)-4-(morpholin-4-yl)pyrimidin-2-yl](phenylsulfonyl)amide

Cited by 3 publications

References 15 publications

Unexpected Products of the Reaction of Cyanoacetylhydrazones of Aryl/heteryl Ketones with Hydrazine: A New Route to Aryl/Heteryl Hydrazones, X-ray Structure, and In vitro Anti-proliferative Activity Against NCI 60-cell Line Panel

Unexpected Products of the Reaction of Cyanoacetylhydrazones of Aryl/heteryl Ketones with Hydrazine: A New Route to Aryl/Heteryl Hydrazones, X-ray Structure, and In vitro Anti-proliferative Activity Against NCI 60-cell Line Panel

Discovery of Promising Sulfadiazine Derivatives With Anti‐Proliferative Activity Against Tumor Cell Lines

Novel synthesis of the first new class of triazine sulfonamide thioglycosides and the evaluation of their anti-tumor and anti-viral activities against human coronavirus

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