synthesis and cytotoxic evaluation of 6-amino-4-aryl-3-methyl-2,4-dihydropyrano[2,3-c]pyrazole-carbonitrile derivatives using borax with potential anticancer effects

a green and efficient one-pot, four-component synthesis of 6-amino-4-aryl-3-methyl-2,4-dihydropyrano[2,3- c ]pyrazo-carbonitrile derivatives catalyzed by borax in water is described. this method provides several advantages such as environmental friendliness, shorter reaction time, excellent yields, and simple workup procedure. the in vitro cytotoxic activity of the synthesized test compounds was investigated against cancer cell lines (sw48, a549, kb, hepg2) in comparison with doxorubicin, a well-known anticancer drug, using mtt colorimetric assay. our compounds showed good and reasonable cytotoxicity than doxorubicin in some studied cell lines. the compounds 5b (2,4-dimethoxy derivative), 5c (3,4,5-trimethoxy derivative), 5g (4-chloro derivative) in kb cell line (ic 50 = 8±2.217 µm, 7±2.77 µm, 7.5± 1.49 µm respectively), 5f (3-chloro derivative) in a549 cell line (ic 50 = 31.5±2.02 µm), 5g (4-chloro derivative) in hepg2 cell line (ic 50 = 22.5±3.09 µm), 5e (2-chloro derivative), and 5i (4-nitro derivative) in sw48 cell line (ic 50 = 23± 0.772 µm, 23± 4.97 µm respectively) showed the best results in close to the control drug.