European Journal of Medicinal Chemistry published new progress about Antitumor agents. 100-70-9 belongs to class nitriles-buliding-blocks, name is Picolinonitrile, and the molecular formula is C6H4N2, COA of Formula: C6H4N2.
Krasavin, Mikhail published the artcileContinued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively kill cancer cells in hypoxic environment, COA of Formula: C6H4N2, the main research area is oxadiazole arenesulfonamide preparation antitumor carbonic anhydrase inhibitor hypoxia SAR; 1,2,4-Oxadiazole; Cancer cells; Carbonic anhydrase; Hypoxic environment; Isoform-selective inhibitors; Isosteric replacement; Periphery groups; Primary sulfonamides; Subnanomolar inhibition.
An expanded set of diversely substituted 1,2,4-oxadiazole-containing primary aromatic sulfonamides I (R1 = cyclopropyl, Ph, 2-MeOC6H4, 3-MeOC6H4, pyridin-2-yl) and II (X = m-phenylene, p-phenylene, thiophene-2,4-diyl, etc.; R2 = Me, cyclopropyl, Ph, thiophen-2-yl, etc.) was synthesized and tested for inhibition of human carbonic anhydrase I, II, IX and XII isoforms. The initial biochem. profiling revealed a significantly more potent inhibition of cancer-related, membrane-bound isoform hCA IX (reaching into submicromolar range), on top of potent inhibition of hCA XII that is another cancer target. The observed structure-activity relationships have been rationalized by mol. modeling. Comparative single-concentration profiling of the carbonic anhydrase inhibitors synthesized for antiproliferative effects against normal (ARPE-19) and cancer (PANC-1) cell lines under chem. induced hypoxia conditions revealed several candidate compounds selectively targeting cancer cells. More in-depth characterization of these leads revealed two structurally related compounds that showed promising selective cytotoxicity against pancreatic cancer (PANC-1) and melanoma (SK-MEL-2) cell lines.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 100-70-9 belongs to class nitriles-buliding-blocks, name is Picolinonitrile, and the molecular formula is C6H4N2, COA of Formula: C6H4N2.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts