A Practical and Eco‐Friendly Synthesis of Stereocontrolled Alkylaminomethylidene Derivatives of 2‐Thiohydantoins by Dimethylamine Substitution.

Chérouvrier, Jean-René; Carreaux, François; Bazureau, Jean Pierre

doi:10.1002/chin.200306129

Cited by 3 publications

(2 citation statements)

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“…2-Thioxoimidazolidin-4-one and its derivatives consist of an important class of heterocyclic compounds due to its wide variety of pharmacological activities as; Hypolipidemic [1] , anti-cancer [2,3] , anti-viral [4,5] , antituberculosis [6] , anti-microbial (anti-fungal and antibacterial) [7] , anti-ulcer and anti-inflammatory [8] .…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Anti-Cancer Evaluation of some Novel Leucettamine B Analouges

Helali

Sarg

Bayoumi

et al. 2023

Journal of Advanced Pharmacy Research

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Objective: Novel anticancer agents were designed to be synthesized considering Leucettamine B as a lead compound. Leucettamine B, which was isolated from a marine sponge, is a tyrosine-regulated inhibitor of kinase 1A (Dyrk1A), and has gained a lot of attention as a pharmacological target in malignant brain tumors. Method: 3-Phenyl-2thioxoimidazolidin-4-one 1 has been used for the synthesis of various fused phenylimidazo2,4]triazine 10-14, 20 and 21 as well as imidazo[1,2b][1,2,4]triazepine analogues 15 and 17 through different chemical reactions. Results: Considering that eleven of the synthesized compounds were selected for evaluation of their anticancer activity by the National Cancer Institute (NCI), U.S.A. The anticancer evaluation was carried out against National Cancer Institute )NCI) cell lines using single high dose. Conclusion: Compounds 8-(4-Methoxybenzylidene)-2,4-diamino-5-phenyl-5H-imidazo[1,2-b][1,2,4,6] tetrazepin-7(8H)one 16, 20 and 24 were found to have selective potent anticancer activity against Non-Small Cell Lung cancer EKVX, Melanoma UACC-62 and Breast cancer HS 578T cell lines.

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Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Anti-Cancer Evaluation of some Novel Leucettamine B Analouges

Helali

Sarg

Bayoumi

et al. 2023

Journal of Advanced Pharmacy Research

View full text Add to dashboard Cite

show abstract

“…2-Thioxoimidazolidin-4-one and its derivatives comprise a class of heterocyclic compounds of valuable importance due to its broad-spectrum pharmacological properties as; hypolipidemic 1 , anticancer 2,3 , antiviral 4,5 , antituberculosis 6 , antimicrobial (antifungal and antibacterial) 7 , anti-ulcer and anti-inflammatory agents 8 .…”

Section: Introductionmentioning

confidence: 99%

Phenylimidazoles Scaffolds as Potent Anticancer Agents (Part I)

Hassan

Sarg²,

Bayoumi³

et al. 2022

Journal of Advanced Pharmacy Research

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Objective: Novel anticancer agents were designed to be synthesized comprising the essential features for anticancer activity considering Leucettamine B as a lead compound. Method: 3-Phenyl-2-thioxoimidazolidin-4-one 1 has been utilized for synthesis of various fused pyrrolo[1,2-e]imidazole 4, 8a,b, 11, 14, 16, 18, 20, 21, 23, 25 analogues through different chemical reactions. Results: Structures of these compounds were confirmed by spectral and elemental analyses Thirteen of the newly synthesized compounds were selected by the NCI -Maryland-U.S.A. and were tested for their anticancer activity in an initial single high dose in the full NCI 60 cell line panel. Conclusion: 5-amino-2,3,7,7a-tetrahydro-7-(4-methoxyphenyl)-1-oxo-2-phenyl-3-thioxo-1H-pyrrolo[1,2-e]imidazole-6-carbonitrile; 4, 1-(7-(4-chlorophenyl)-3,7dihydro-1,5-dihydroxy-2-phenyl-3-thioxo-2H-pyrrolo[1,2-e]imidazol-6yl) ethenone; 21, were found to possess very selective potent anticancer activity against certain cancer cell lines.

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DMF-DMA catalyzed Synthesis, molecular docking, in-vitro, in-silico design, and binding free energy studies of novel thiohydantoin derivatives as antioxidant and antiproliferative agents targeting EGFR tyrosine kinase and aromatase cytochrome P450 enzyme

Seliem

2024

Bioorganic Chemistry

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A Practical and Eco‐Friendly Synthesis of Stereocontrolled Alkylaminomethylidene Derivatives of 2‐Thiohydantoins by Dimethylamine Substitution.

Cited by 3 publications

References 1 publication

Design, Synthesis, and Anti-Cancer Evaluation of some Novel Leucettamine B Analouges

Design, Synthesis, and Anti-Cancer Evaluation of some Novel Leucettamine B Analouges

Phenylimidazoles Scaffolds as Potent Anticancer Agents (Part I)

DMF-DMA catalyzed Synthesis, molecular docking, in-vitro, in-silico design, and binding free energy studies of novel thiohydantoin derivatives as antioxidant and antiproliferative agents targeting EGFR tyrosine kinase and aromatase cytochrome P450 enzyme

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