Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines

Nornostocine congeners as potential anticancer drugs: An overview

“…Compounds 5a and 5b exhibited comparatively higher activity against leukemia (K532, BV173; Bcr‐Abl positive) cell lines and decreased the phosphorylation of STAT5. Both compounds inhibited reactions against Abl kinase with IC 50 values, 5.8 and 5.9 μM, respectively (Mojzych et al, ).…”

“…These compounds were synthesized by reacting the intermediate compound 1‐benzyl/methyl‐5‐hydrazino‐3‐methyl‐1 H ‐pyrazolo[4,3‐ e ][1,2,4]triazine with aqueous solution of sodium nitrite in acetic acid at low temperature to liberate corresponding 5‐azido derivatives 2a and 2b . Moreover, two possible fused ring systems 3a and 3b were obtained by treatment with hot ethanol of 2a and 2b (Mojzych, Šubertová, et al, ). As reported, the two compounds had good yields individually.…”

New pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors

“…17 On the other hand, naturally occurring pyrazolo [4,3-e] [1,2,4]triazines are a very important group of heterocyclic compounds in the medicinal chemistry due to their anticancer and antibacterial activity. 18 Moreover our recent structure-activity relationship study on pyrazolo [4,3-e] [1,2,4]triazine sulfonamides demonstrated that the certain within this series are potent kinase inhibitors and exhibit antileukemic activity in vitro 19 and are effective against the tumor-associated CA IX and XII. 20 In our current work, continuing our interest in sulfonamides as carbonic anhydrase inhibitors, and considering sildenafil analogues as lead molecules, 19,20 we have synthesized new mono-and disulfonamides.…”

“…18 Moreover our recent structure-activity relationship study on pyrazolo [4,3-e] [1,2,4]triazine sulfonamides demonstrated that the certain within this series are potent kinase inhibitors and exhibit antileukemic activity in vitro 19 and are effective against the tumor-associated CA IX and XII. 20 In our current work, continuing our interest in sulfonamides as carbonic anhydrase inhibitors, and considering sildenafil analogues as lead molecules, 19,20 we have synthesized new mono-and disulfonamides. We were interested to see whether replacement of the methyl group at position N1 of the heterocyclic nucleus with the aryl substituent has important consequences for anticancer activity and for the interaction of these sulfonamides with the various CA isoforms, such as CA I, II, IX and XII.…”

Design, synthesis, and biological activity of phenyl-pyrazole derivatives as BCR–ABL kinase inhibitors

“…Consequently, there is still necessary to discovery new compounds that will enrich the pool of known tyrosine kinase inhibitors. 12 So far, several cocrystal structures of BCR-ABL kinase with their inhibitors have been reported. These inhibitors possessed some key structural elements which formed crucial interactions between the protein and inhibitors base on of structural analysis of the inhibitors (i.e., imatinib and ponatinib) and BCR-ABL kinase.…”