Selectivity in domino reaction of ortho-carbonyl azides with malononitrile dimer leading to [1,2,3]triazolo[1,5-a]pyrimidines

Anticancer activity evaluation of thieno[3,2-e][1,2,3]triazolo[1,5-a]pyrimidines and thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine derivatives

“…The thienotriazolopyrimidine derivatives were designed as promising anticancer agents and obtained as we described earlier [16,21,12].…”

“…Moreover, we previously synthesized several 1,2,3-triazoles which were found to possess significant anticancer activity [10,11]. Recently, we have developed facile synthetic methods for the versatile synthesis of 1,2,3-triazole and thieno-fused compounds, where new efficient and mild procedures from readily available reagents can be employed [12][13][14][15][16][17][18][19][20][21][22][23][24][25][26]. Those protocols could be successfully used for the preparation of fused heterocyclic compounds with both thiophene and 1,2,3-triazole rings.…”

“…Based on such combination an extended structure-activity investigation focusing on drug-like properties should be performed. The present work is devoted to the evaluation of anticancer activity of substituted thienotriazolopyrimidines synthesized at room temperature in a short time via domino-1,3-dipolar cyclocondensation [16,21,12] that meets the energy-saving and environmentally friendly philosophical concepts of 'green chemistry'. The point of the research was to perform in vitro anticancer activity assay of the fused substituted thienotriazolopyrimidines.…”

Synthesis of novel 3-(1,2,4-oxadiazol-5-yl)thiophen-2-amine derivatives via gewald reaction

“…Our previous studies on aminothiophenes established some convenient chemical modifications of the Gewald 2-aminothiophenes and isomeric 3-aminothiophenes, the scope of their synthetic application in various fused nitrogen containing heterocycles preparation ____________________  Shyyka O., Svyrydenko M., Tupychak M. et al, 2021 in energy-saving and environmentally friendly manner was also determined [11][12][13][14][15][16][17][18][19]. Such approaches allowed to create broad combinatorial libraries for drug discovery and to select drug-like examples possessing significant anticancer activity [20][21][22].…”

Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents

“…Various 5-amino-1,2,3-triazoles were obtained by using an efficient synthetic method from the [12,13], 1,3-thiazole [14,15], 1,2,4-/1,3,4-oxadiazole [14], pyrroles and indoles [16] rings and with possible the simultaneous cascade processes leading to polycyclic systems [17,18]. Additionally, the azide [3 + 2] cycloadditions can be performed at room temperature in good to excellent yields of products in the presence of catalytic amounts of pyrrolidine (5-10 mol%) [19,20] according to organocatalytic methodology [21][22][23][24].…”