Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents

A series of new 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydro quinazolinone hybrids with different linker architectures have been designed and synthesized. These compounds have been evaluated for their anticancer activity. One of the compounds 4c amongst this series has shown promising anticancer activity. Further some detailed biological assays relating to the cell cycle aspects and tubulin depolymerization activity have been examined with a view to understand the mechanism of action of this conjugate.

Graphical abstractNew class of 3,5-diaryl isoxazoline/isoxazole linked 2,3-Dihydroquinazolinone hybrids were prepared and evaluated for anticancer activity. Some of the biological assays were also carried out for the most potent compound 4c.Figure optionsDownload full-size imageDownload as PowerPoint slideResearch highlights► G2/M arrest in MCF-7 cell lines. ► Disruption of microtubules as well as fragmentation of nuclei. ► G2/M arrest associated with cyclins and CDKs. ► Cleavage of PARP leads to DNA damage and cell death of MCF-7 cell lines.