Synthesis and antitumor properties of derivatives 4-substituted-5-(piridin-4-yl)-4h-1,2,4-triazole-3-thiol

Rusnac Roman; Zatic Ana; Paholnitscaia Anastasia; Barba Nicanor; Perreault M.; Gulya Aurelian

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2023-05-29 14:19

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RUSNAC, Roman, ZATIC, Ana, PAHOLNITSCAIA, Anastasia, BARBA, Nicanor, PERREAULT, M., GULYA, Aurelian. Synthesis and antitumor properties of derivatives 4-substituted-5-(piridin-4-yl)-4h-1,2,4-triazole-3-thiol. In: Physical Methods in Coordination and Supramolecular Chemistry, 8-9 octombrie 2015, Chişinău. Chisinau, Republic of Moldova: 2015, XVIII, p. 131.

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Physical Methods in Coordination and Supramolecular Chemistry
XVIII, 2015

Conferința ""Physical Methods in Coordination and Supramolecular Chemistry""
Chişinău, Moldova, 8-9 octombrie 2015

Synthesis and antitumor properties of derivatives 4-substituted-5-(piridin-4-yl)-4h-1,2,4-triazole-3-thiol

Pag. 131-131

Rusnac Roman¹, Zatic Ana¹, Paholnitscaia Anastasia¹, Barba Nicanor¹, Perreault M.², Gulya Aurelian¹

¹ Moldova State University,
² CHUL Research Center (Université Laval)

Teze de doctorat:

Raportat: Sinteza dirijată și proprietățile biologice ale complecșilor de Cu(II) cu 2- hidrazinobenzotiazol și 4-morfolintiosemicarbazone

Disponibil în IBN: 22 aprilie 2020

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In recent years, the chemistry of triazoles and their fused heterocyclic derivatives has received considerable attention owing to their synthetic and effective biological importance [1]. Literature survey reveals that 1,2,4-triazole derivatives exhibit a wide range of biological activities including Antibacterial, Antifungal, Antitumour, Anti-inflammatory, Antitubercular, Hypoglycemic, Antidepressant, Anticonvulsant, Anticancer, Antimalarial, Antiviral, Antiproliferative, Analgesic and Antimigraine [1,2]. The derivatives of 4-substituted-5(piridin-4-yl)-4H-1,2,4-triazole-3-thiol were synthesized according to scheme:schemeTable. The antiproliferative activity of 4-substituted-5-(piridin-4-yl)-4H-1,2,4-triazole-3-thiol on human on leukemia (HL-60) cells.tableThe obtained data demonstate that the synthesized compounds show moderate (3-11%) antiproliferative activity. Compounds e and d were tested on melanoma (MeW-164) and on human leukemia (HL-60) cells, in the range of (0,1-10 μM) concentrations. The results proved thait they have a higher (16-23%) antiproliferative activity.

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<description xml:lang='en' descriptionType='Abstract'><p>In recent years, the chemistry of triazoles and their fused heterocyclic derivatives has received considerable attention owing to their synthetic and effective biological importance [1]. Literature survey reveals that 1,2,4-triazole derivatives exhibit a wide range of biological activities including Antibacterial, Antifungal, Antitumour, Anti-inflammatory, Antitubercular, Hypoglycemic, Antidepressant, Anticonvulsant, Anticancer, Antimalarial, Antiviral, Antiproliferative, Analgesic and Antimigraine [1,2]. The derivatives of 4-substituted-5(piridin-4-yl)-4H-1,2,4-triazole-3-thiol were synthesized according to scheme:</p><p>scheme</p><p>Table. The antiproliferative activity of 4-substituted-5-(piridin-4-yl)-4H-1,2,4-triazole-3-thiol on human on leukemia (HL-60) cells.</p><p>table</p><p>The obtained data demonstate that the synthesized compounds show moderate (3-11%) antiproliferative activity. Compounds e and d were tested on melanoma (MeW-164) and on human leukemia (HL-60) cells, in the range of (0,1-10 &mu;M) concentrations. The results proved thait they have a higher (16-23%) antiproliferative activity.</p><p>&nbsp;</p></description>
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