Multi-component synthesis and in vitro and in vivo anticancer activity of novel arylmethylene bis-isoxazolo[4,5-b]pyridine-N-oxides

A three component one-pot protocol has been investigated for the synthesis of arylmethylene bis-isoxazolo[4,5-b]pyridine-N-oxides 1 from the commercially available materials. The title compounds 1 were also synthesized by a step-wise method and found to be identical with one-pot synthesis by spectral and analytical data. The newly synthesized compounds were evaluated for their in vitro anticancer activity against human cancer cell lines and in vivo anticancer activity on EAC-bearing mice. Compound 1a was found to be the most active both in in vitro and in vivo cytotoxic studies.

Graphical abstractMulti-component synthesis of novel arylmethylene bis-isoxazolo[4,5-b]pyridine-N-oxides and their in vitro and in vivo anticancer activity was reported.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Novel arylmethylene bis-isoxazolo[4,5-b]pyridine-N-oxides. ► Multi-component one-pot synthesis. ► In vitro and In vivo anticancer activity. ► Compounds 1a and 1h showed good in vivo anticancer activity.