Synthesis of N-sulfonated aziridines

Elgemeie, Galal H.; Azzam, Rasha A.; Zaghary, Wafaa A.; Aly, Ashraf A.; Metwally, Nadia H.; Sarhan, Mona O.; Abdelhafez, Elshimaa M.; Elsayed, Rasha E.

doi:10.1016/b978-0-12-822179-2.00006-9

Cited by 2 publications

(1 citation statement)

References 111 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…We are currently developing several synthetic strategies for the preparation of new heterocyclic compounds containing Nsulfonylamino-and N-sulfonyl moieties, which have recently been shown to possess significant biological activity as novel anti-covid-19, antimicrobial and antiviral agents (Azzam et al, 2019;Elgemeie et al, 2019Elgemeie et al, , 2022Zhu et al, 2013). Some of our recently reported N-arylsulfonylpyrazoles (Elgemeie et al, 1998(Elgemeie et al, , 2002(Elgemeie et al, , 2013 have been used by other groups as inhibitors of NS2B-NS3 virus and cathepsin B16 Sidique et al, 2009).…”

Section: Chemical Contextmentioning

confidence: 99%

Crystal structure of 2-[(5-amino-1-tosyl-1H-pyrazol-3-yl)oxy]-1-(4-methoxyphenyl)ethan-1-one 1,4-dioxane monosolvate

Metwally,

Elgemeie,

Jones

2024

Acta Cryst E

Self Cite

View full text Add to dashboard Cite

In the structure of the title compound, C19H19N3O5S·C4H8O2, the two independent dioxane molecules each display inversion symmetry. The pyrazole ring is approximately parallel to the aromatic ring of the oxy-ethanone group and approximately perpendicular to the tolyl ring of the sulfonyl substituent. An extensive system of classical and `weak' hydrogen bonds connects the residues to form a layer structure parallel to (201), within which dimeric subunits are conspicuous; neighbouring layers are connected by classical hydrogen bonds to dioxanes and by `weak' hydrogen bonds from Htolyl donors.

show abstract

Section: Chemical Contextmentioning

confidence: 99%

Crystal structure of 2-[(5-amino-1-tosyl-1H-pyrazol-3-yl)oxy]-1-(4-methoxyphenyl)ethan-1-one 1,4-dioxane monosolvate

Metwally,

Elgemeie,

Jones

2024

Acta Cryst E

Self Cite

View full text Add to dashboard Cite

show abstract

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

Mohamed‐Ezzat,

Kariuki,

Azzam

2024

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

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.

show abstract

Synthesis of N-sulfonated aziridines

Cited by 2 publications

References 111 publications

Crystal structure of 2-[(5-amino-1-tosyl-1H-pyrazol-3-yl)oxy]-1-(4-methoxyphenyl)ethan-1-one 1,4-dioxane monosolvate

Crystal structure of 2-[(5-amino-1-tosyl-1H-pyrazol-3-yl)oxy]-1-(4-methoxyphenyl)ethan-1-one 1,4-dioxane monosolvate

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

Contact Info

Product

Resources

About