ChemInform Abstract: Synthesis of Some New 1,6‐Dihydro‐3‐substituted 6‐Spiro‐(9′‐fluorene)‐ 1,2,4‐triazin‐5‐(4H)‐ones as Potential Anti HIV and Anticancer Drugs.

Abdel‐Rahman, Reda M.; Seada, M.; Fawzy, M. H.; El‐Baz, I.

doi:10.1002/chin.199512225

Cited by 4 publications

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“…Reumycin [ 24 ] is isolated from actinomyces rectus bruneus and used as an antitumor antibiotic for treating brain tumors. Other hetero annelated 1,2,4-triazines have clinical antiviral effect against influenza A and B viruses [ 4 ], anti-HIV and anticancer activity [ 5 , 6 ]. They also show antimicrobial, antifungal effects and cytotoxicity to MCF-7 cells [ 7 , 8 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and anticancer evaluation of some novel pyrimido[5,4-e][1,2,4]triazines and pyrazolo[3,4-d]pyrimidine using DMF-DMA as methylating and cyclizing agent

El‐Kalyoubi

2018

Chemistry Central Journal

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BackgroundDescribed a series of main target compounds pyrimido[5,4-e][1,2,4]triazines is obtained via condensation of 6-hydrazinyluracil with different aromatic aldehydes to give the hydrazones followed by nitrosation with HNO2 then intramolecular cyclization. On the other hand, pyrazolopyrimidines can be obtained by the reaction of hydrazones with dimethylformamide-dimethylacetal (DMF-DMA), DMF-DMA in the presence of DMF or by refluxing the hydrazinyluracil with DMF-DMA in the presence of DMF directly. The newly synthesized compounds are evaluated in vitro for their anticancer activity against human lung carcinoma (A549).ResultsA newly substituted compounds of benzaldehyde-pyrimidin-4-yl)hydrazones (5a–f), pyrimido[5,4-e][1,2,4]triazines 6a–e, arylethylidenehydrazinylpyrimidine 7a,b and pyrazolopyrimidines 9,11 are screened for cytotoxic activity against human lung carcinoma (A549) cell line. They exhibited a good yield. Compound 6b shows the highest effect with IC50 value 3.6 μM, followed by compounds 9, 5a, 8, 5e, 6e, 5b, 5f, 7a, 5c, 6c, 7b, 6a, 11, 5d and 6d.ConclusionA simple and efficient route is used for the synthesis of pyrimido[5,4-e][1,2,4]triazines and pyrazolopyrimidines. The synthesized compounds are screened for antitumor activity.

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Section: Introductionmentioning

confidence: 99%

Synthesis and anticancer evaluation of some novel pyrimido[5,4-e][1,2,4]triazines and pyrazolo[3,4-d]pyrimidine using DMF-DMA as methylating and cyclizing agent

El‐Kalyoubi

2018

Chemistry Central Journal

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“…In addition, BX-1382BS (V) showed a significant activity as protein kinase inhibitor [26] and a cyanopyrimidine scaffold JNJ-17029259 (VI) is an oral inhibitor of VEGF-mediated signal transduction [27] (Figure 1). Recently a great deal of synthetic efforts has been spent on fluorinated uncondensed 1,2,4-triazines by our group searching for new anti-HIV and anticancer agents [28][29][30][31][32][33][34][35][36][37][38] (compounds A-F; Figure 2).…”

Section: Introductionmentioning

confidence: 99%

Fluorine Substituted 1,2,4-Triazinones as Potential Anti-HIV-1 and CDK2 Inhibitors

Makki

Abdel‐Rahman

Khan

2014

Journal of Chemistry

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Fluorine substituted 1,2,4-triazinones have been synthesized via alkylation, amination, and/or oxidation of 6-(2-amino-5-fluorophenyl)-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one 1 and 4-fluoro-N-(4-fluoro-2-(5-oxo-3-thioxo-2,3,4,5-tetrahydro-1,2,4-triazin-6-yl)phenyl)benzamide 5 as possible anti-HIV-1 and CDK2 inhibitors. Alkylation on positions 2 and 4 in 1,2,4triazinone gave compounds 6-8. Further modification was performed by selective alkylation and amination on position 3 to form compounds 9-15. However oxidation of 5 yielded compounds 16-18. Structures of the target compounds have been established by spectral analysis data. Five compounds (5, 11, 14, 16, and 17) have shown very good anti-HIV activity in MT-4 cells. Similarly, five compounds (1, 3, and 14-16) have exhibited very significant CDK2 inhibition activity. Compounds 14 and 16 were found to have dual anti-HIV and anticancer activities.

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“…1,2,4-Triazines have gained considerable pharmacological interest due to their anticonvulsant [4,5], anticancer [6][7][8][9], antiprotozoal [10], anti-viral [11], anti-malarial [12], antibacterial [13][14][15] and antifungal effects [16][17][18]. In the field of agriculture, they showed effects such as insecticides, herbicides, plant growth regulators and they are deployed for enhancing crop yield [19][20][21].…”

Section: Introductionmentioning

confidence: 99%

5-[(5-Chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene]-2-(4-nitrobenzoyl)-3-phenyl-2,5-dihydro-1,2,4-triazin-6(1H)-one

Kaushik¹,

Verma²

2011

Molbank

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ChemInform Abstract: Synthesis of Some New 1,6‐Dihydro‐3‐substituted 6‐Spiro‐(9′‐fluorene)‐ 1,2,4‐triazin‐5‐(4H)‐ones as Potential Anti HIV and Anticancer Drugs.

Cited by 4 publications

References 0 publications

Synthesis and anticancer evaluation of some novel pyrimido[5,4-e][1,2,4]triazines and pyrazolo[3,4-d]pyrimidine using DMF-DMA as methylating and cyclizing agent

Synthesis and anticancer evaluation of some novel pyrimido[5,4-e][1,2,4]triazines and pyrazolo[3,4-d]pyrimidine using DMF-DMA as methylating and cyclizing agent

Fluorine Substituted 1,2,4-Triazinones as Potential Anti-HIV-1 and CDK2 Inhibitors

5-[(5-Chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene]-2-(4-nitrobenzoyl)-3-phenyl-2,5-dihydro-1,2,4-triazin-6(1H)-one

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