ChemInform Abstract: Synthesis of Some New Heterobicyclic Nitrogen Systems Bearing the 1,2,4‐Triazine Moiety as Anti‐HIV and Anticancer Drugs. Part 2.

Abdel‐Rahman, Reda M.; Morsy, J. M.; El-Edfawy, Somaya M.; Amine, H. A.

doi:10.1002/chin.200002175

Cited by 13 publications

(12 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A number of 1,2,4-triazinone derivatives possess significant biological activities, such as antimicrobial, fungicide, pesticide, herbicide and crop protection agents, as well as blood platelet aggregation-inhibition (Neunhoeffer et al, 1978;El Ashry et al, 1994;Abdel-Rahman, 2001), while some others exhibit anti-HIV and antitumoral activity against leukemia, ovarian cancer, small and large lung cancer cells, and breast cancer (Abdel-Rahman et al, 1999;El-Gendy et al, 2001;Krauth et al, 2010). Among the different 1, 2, 4-triazinones described in the literature, only a few are 4,5-dihydro-1,2,4-triazin-6-ones 1-4 ( Fig.1) (El-Abadelah et al,1991;Dalloul et al, 2008;Collins et al, 1996;El-Abadelah et al, 1997).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Fluorogenic Properties of Some 1-(Coumarin-7-yl)-4,5-dihydro-1,2,4-triazin-6(1H)-ones

Mustafa¹,

El‐Abadelah²,

Mubarak³

et al. 2011

IJC

View full text Add to dashboard Cite

Herein, we have synthesized and tested a selected set of N1-(coumarin-7-yl)-4,5-dihydro-1,2,4-triazin-6(1H)-ones (8) incorporating masked α-amino acids within the triazinone skeleton as synthetic fluorogenic substrates for amino peptidases using human nasal epithelium that expressed aminopeptidases. These chiral triazinones, obtained via direct interaction of α-amino esters with N1-(coumarin-7-yl) nitrile imine (generated in situ from its hydrazonoyl chloride by the action of triethylamine), bear close resemblance to 7-amino-4-methylcoumarin (AMC) with labeled α-amino acids (AA-AMC's/7). The aminopeptidase activity of the synthesized compounds (0.125 and 0.5 mM) was compared with that of a model compound L-alanine-4-methylcoumaryl-7-amide (Ala-MCA), following in-house validation of the aminopeptidase activities of the human nasal primary culture. In comparison to the model aminopeptidase substrate (Ala-MCA), the synthesized compounds yielded fluorescent 7-amino-4-methylcoumarin following incubation with nasal epithelial cells. However, the yield was significantly lower than was observed for the control compound.

show abstract

Section: Introductionmentioning

confidence: 99%

Synthesis and Fluorogenic Properties of Some 1-(Coumarin-7-yl)-4,5-dihydro-1,2,4-triazin-6(1H)-ones

Mustafa¹,

El‐Abadelah²,

Mubarak³

et al. 2011

IJC

View full text Add to dashboard Cite

show abstract

“…In addition, triazolopyridines are also interesting compounds due to their pronounced biological activity, as they can be used as antidepressants [11][12][13]. Various pyridine derivatives are well known to possess an array of physiological activities, such as anticancer, muscle relaxant, hypnotic, antiinflammatory, diuretic, and antihypertensive activities [14][15][16][17]. Imidazole derivatives are part of anticancer drugs like mercaptopurine.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and anticancer activity of some new pyridine derivatives

et al. 2011

View full text Add to dashboard Cite

Different substituents were introduced in positions 2 and 6 of 2,6 diaminopyridine in order to obtain new heterocyclic compounds. A new series of aza pyridine, imidazopyridine, benzodiazepine, indole, pyrimidine, and benzimidazole heterocyclic derivatives were synthesized in good yields. The anticancer activities of some of the new compounds were evaluated against liver cancer cell line HEPG2. Compounds 3, 4, 10, 11, 12, and 17 showed the highest activity when compared to 5-flurouracil (5-FU) and doxorubicin (DOX) chemotherapy.

show abstract

“…Many 1,2,4-triazine derivatives are well known to possess biological activities. 2,3 Over the last two decades asymmetric triazines have been screened in vitro supporting their anticancer, [4][5][6] anti-HIV [4][5][6] and tuberculostatic activities. 7 Pyrimido [1,2,4]triazines show interesting biological activities, such as the antibiotics toxoflavine, reumycine, fervenuline and methylfervenuline all possessing a pyrimido [5,4-e][1,2,4]triazine (7-azapteridine) system.…”

Section: Introductionmentioning

confidence: 99%

Analogs of biologically active compounds IX. Synthesis of several new uracil and pteridine 6-aza-analogs based on cyclization of arylhydrazones derived from mesoxalic acid

Novosd¹,

Stskala²

2017

Arkivoc

View full text Add to dashboard Cite

A series of 5C and 5N substituted 3-oxo-2-phenyl-1,2,4-triazine-6-carbonitriles and 8-imino-2-arylpyrimido [4,5-e] [1,2,4]triazine-3,6(2H,5H)-diones (6-aryl-6-azapteridines) are described via a cyclocondensation reaction from the corresponding aryliminohydrazones with CDI. The required aryliminohydrazones were obtained from the starting compound -malononitrile. These prepared compounds were tested for cytotoxic activity on cancer cell lines.

show abstract

ChemInform Abstract: Synthesis of Some New Heterobicyclic Nitrogen Systems Bearing the 1,2,4‐Triazine Moiety as Anti‐HIV and Anticancer Drugs. Part 2.

Cited by 13 publications

References 0 publications

Synthesis and Fluorogenic Properties of Some 1-(Coumarin-7-yl)-4,5-dihydro-1,2,4-triazin-6(1H)-ones

Synthesis and Fluorogenic Properties of Some 1-(Coumarin-7-yl)-4,5-dihydro-1,2,4-triazin-6(1H)-ones

Synthesis and anticancer activity of some new pyridine derivatives

Analogs of biologically active compounds IX. Synthesis of several new uracil and pteridine 6-aza-analogs based on cyclization of arylhydrazones derived from mesoxalic acid

Contact Info

Product

Resources

About