A series of novel isoxazole functionalized pyrazolo[3,4‐b]pyridine derivatives 5a‐n were prepared, respectively, initiated from 6‐thiophenyl‐4‐(trifluoromethyl)‐1H‐pyrazolo[3,4‐b]pyridin‐3‐amine 3 through selective N‐propargylation, and these N‐propargylated compounds 4 were cyclized with aryloximes by using of sodium hypochlorite, and obtained the title products 5a‐n. All the final products 5a‐n were submitted for anticancer activity against four cancer cell lines such as “HeLa—cervical cancer (CCL‐2); COLO 205—colon cancer (CCL‐222); HepG2—liver cancer (HB‐8065); MCF7—breast cancer (HTB‐22)”; Compounds 5c, 5d, and 5h are found to have more prominent anticancer activity at micro molar concentration.
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