Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents

Ma, Liying; Pang, Liuqing; Wang, Bo; Zhang, Miao; Hu, Biao; Xue, Deng‐Qi; Shao, Kun‐Peng; Zhang, Baole; Liu, Ying; Zhang, En; Liu, Hong‐Min

doi:10.1016/j.ejmech.2014.08.010

Cited by 103 publications

(47 citation statements)

References 39 publications

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“…Elemental analysis was undertaken with Elemental Vario EL III Carlo Erba 1108 analyser. Syntheses of the target compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12) were performed according to fig. 2, through following steps.…”

Section: Methodsmentioning

confidence: 99%

“…Triazole heterocycles is a building block of great value in drug candidates [8,9] and a large number of ring systems containing this heterocyclic core have been incorporated into a wide variety of therapeutically interesting drug compounds including antiinflammatory, CNS stimulants, sedatives, antianxiety [10,11] and antimycotic agents such as fluconazole, itraconazole and voriconazole [12,13] . The 1,2,4-triazole, as well found to exhibit antiasthmatic [14] , antiviral (ribavirin) [15] , antifungal (fluconazole) [16] , antimicrobial [17,18] , antibacterial [19][20][21] , insecticidal [22] , hypnotic [23] , cytotoxic [24] , antitubercular [25] and hypotensive [26,27] activities.…”

Section: Research Papermentioning

confidence: 99%

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Design and Synthesis of New Bioactive 1,2,4-Triazoles, Potential Antitubercular and Antimicrobial Agents

Singh¹,

Kashaw²,

Mishra³

et al. 2018

pharmaceutical-sciences

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Section: Methodsmentioning

confidence: 99%

Section: Research Papermentioning

confidence: 99%

Design and Synthesis of New Bioactive 1,2,4-Triazoles, Potential Antitubercular and Antimicrobial Agents

Singh¹,

Kashaw²,

Mishra³

et al. 2018

pharmaceutical-sciences

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“…As shown in Scheme 3, 5,6-diaryl-1,2,4-triazine-triazole derivatives 11A–11L were achieved by reaction of compound 10B with various azides [25, 26] using sodium ascorbate and CuSO 4 .5H 2 O in THF at room temperature. The structures of all the new synthesized compounds 10A–10C and 11A–11L were characterized by 1 H NMR、 13 C NMR and HRMS.…”

Section: Resultsmentioning

confidence: 99%

Discovery of 5,6-diaryl-1,2,4-triazines hybrids as potential apoptosis inducers

Song

Hou

et al. 2017

European Journal of Medicinal Chemistry

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A series of 5,6-diaryl-1,2,4-triazines hybrids bearing a 1,2,3-triazole linker were synthesized by molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, EC-109 and PC-3). The first structure-activity relationship (SAR) for these 5,6-diaryl-1,2,4-triazines is explored in this report with evaluation of 15 variants of the structural class. Among these chemical derivatives, 3-(((1-(4-fluorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)thio)-5,6-diphenyl-1,2,4-triazine (11E) showed the more potent inhibitory effect against three cell lines than 5-Fu. Cellular mechanism studies in MGC-803 cells elucidated 11E inhibited colony formation and arrested cell cycle at G2/M phase. Furthermore, compound 11E caused morphological changes, decreased mitochondrial membrane potential, and induced apoptosis through the apoptosis-related proteins in MGC-803 cells. It was the first time, to our knowledge, that 5,6-diaryl-1,2,4-triazines bearing a 1,2,3-triazole linker were used as potential apoptosis inducers.

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“…They have been reported to be antagonists and agonists of receptors [19][20][21] , inhibitors of enzymes 22 , and were found to exhibit antihistaminic, cytotoxic, neuroleptic, anti proliferative and anti-hiv-1 activities [23][24][25][26][27] as well as their antimicrobial, antitumor, antibacterial, antiinflammatory, antiviral and antifungal agents [28][29][30][31][32][33][34] .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Anti-Inflammatory Activity of Hydrazide-Hydrazones Bearing Anacardic Acid and 1,2,3-Triazole Ring Based Hybrids

Reddy¹,

Kathale²

2017

Orient. J. Chem

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A novel series of hydrazide-hydrazone derivatives 39-50, linked with anacardic acid motif and 1,2,3-triazole ring were synthesized by reacting 4-(1-(2-methoxy-6-pentadecylbenzyl)-1H-1, 2, 3-triazol-4-yl)benzaldehyde with 2-phenyl-acetohydrazides and benzohydrazides. The structures of the newly synthesized hydrazide-hydrazone derivatives 39-50 were confirmed by 1 H NMR, MS and IR spectroscopic tools. These compounds were also evaluated for their anti-inflammatory activity by carrageenan paw edema method.

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Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents

Cited by 103 publications

References 39 publications

Design and Synthesis of New Bioactive 1,2,4-Triazoles, Potential Antitubercular and Antimicrobial Agents

Design and Synthesis of New Bioactive 1,2,4-Triazoles, Potential Antitubercular and Antimicrobial Agents

Discovery of 5,6-diaryl-1,2,4-triazines hybrids as potential apoptosis inducers

Synthesis and Anti-Inflammatory Activity of Hydrazide-Hydrazones Bearing Anacardic Acid and 1,2,3-Triazole Ring Based Hybrids

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