Synthesis, anticancer activity and molecular modeling studies of 1,2,4-triazole derivatives as EGFR inhibitors

El-Sherief, Hany A.M.; Youssif, Bahaa G.M.; Bukhari, Syed Nasir Abbas; Abdelazeem, Ahmed H.; Abdel‐Aziz, Mohamed; Abdel‐Rahman, Hamdy M.

doi:10.1016/j.ejmech.2018.07.024

Cited by 141 publications

(61 citation statements)

References 32 publications

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“…Aza-heterocycles are amongst the medications which have diverse uses in the market (Figure 1). Of this class, 1,2,4-triazines [7][8][9][10][11][12][13] and 1,2,4-triazoles [14][15][16][17][18][19][20][21], as well as pyrimidines [22,23], have been introduced in a renewed generation of medication. Due to our interest in these azines, their ligation, and modification, we revisited and continued upon our previous research projects [24][25][26][27][28][29][30] with this study.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Azab

Elkanzi

2020

Molecules

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A series of 34 new pyrimido[2,1-c] [1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the conjugates 15a and 15f-j that were tagged with electron-withdrawing groups, with sensitivities ranging from 77% to as high as 100% of the positive control. The investigation of antimicrobial activity included Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6535, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 8739 (EC), and fungal strains Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404.

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Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Azab

Elkanzi

2020

Molecules

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“…Considering that 1 showed significant toxicity in glioma and breast cancer cells, we performed in silico studies with induced fit molecular docking approach. With reference to previous reports on triazole containing molecules, we selected 16 protein targets associated with different cancers of brain, breast and colon . The docking results are presented in Table , which includes docking scores, RMSD values of re‐docked and co‐crystallized ligands, MM‐GB/SA dG bind energies, and amino acid residues involved in hydrogen bonding with the acyclic nucleoside 1 .…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Anti‐Proliferative Activity of a Triazole‐Fused Thymidine Analogue

et al. 2020

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Here we report the synthesis of two-an acyclic and a macrocyclic-analogues of thymidine linked to a triazole moiety. The new molecules were synthesized through an intramolecular 1,3-dipolar cycloaddition reaction of the diazido derivative of thymidine with a suitable alkyne. The acyclic nucleoside showed dose dependent cytotoxicity against glioblastoma and breast cancer cells by causing significant cellular damage as studied with confocal laser scanning microscopy. In silico induced fit molecular docking studies showed poly(ADP-ribose) polymerase 1 (PARP1) as a potential target of the acyclic nucleoside. On the other hand, both the analogues showed no toxicity against normal fibroblast cells. ChemistrySelectCommunications

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“…El‐Sherief et al synthesized derivatives of 1,2,4‐triazole ( 35 ) (Figure ) and examined them for anticancer activity. Among this series of compounds, 35d (IC 50 = 1.60 μM) bearing a combination of electron‐donating triazole and electron‐withdrawing thiazole exhibited potent activity against cancer cell growth and epidermal growth factor recetor.…”

Section: Pharmacological Applications Of 124‐triazolementioning

confidence: 99%

Exploring recent developments on 1,2,4‐triazole: Synthesis and biological applications

Sathyanarayana

Poojary

2020

J Chinese Chemical Soc

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Triazoles are nitrogen-bearing heterocycles. In the last few decades, researchers have focused on fused heterocycles, as they have better pharmacological effect compared to triazoles alone. Among the two isomers of triazole, this article aims to explore the work carried out on 1,2,4-triazole and N-bridged heterocycles derived from 1,2,4-triazole in last 18 years, highlight different synthetic pathways, and present a brief summary of the different biological activities possessed by 1,2,4-triazole derivatives. The information collected in this article is expected to help researchers to discover novel therapeutic agents for better applications in the field of pharmaceutical science. K E Y W O R D Sbio-organic chemistry, medicinal chemistry, organic chemistry

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Synthesis, anticancer activity and molecular modeling studies of 1,2,4-triazole derivatives as EGFR inhibitors

Cited by 141 publications

References 32 publications

Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Synthesis and Anti‐Proliferative Activity of a Triazole‐Fused Thymidine Analogue

Exploring recent developments on 1,2,4‐triazole: Synthesis and biological applications

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