Docking studies, synthesis, characterization of some novel oxazine substituted 9-anilinoacridine derivatives and evaluation for their antioxidant and anticancer activities as topoisomerase II inhibitors

A series of 9-anilinoacridines substituted with oxazine derivatives were synthesized to evaluate their antioxidant and anticancer activity against Daltons Lymphoma Ascites (DLA) cell growth by in vitro method. It was revealed that these conjugates exhibited significant antioxidant and anticancer activity (inhibition of DLA cell proliferation). Among these agents, compounds 5a, 5h, 5i, 5j were the most cytotoxic with CTC50 value of 140–250 μg/mL. The docking studies of the synthesized compounds were performed towards the key Topoisomerase II (1QZR) by using Schrodinger Maestro 9.2 version. The oxazine substituted 9-anilinoacridine derivatives 5a, 5h, 5i, 5j have significant anticancer activity as topoisomerase II inhibitors.

Graphical abstractSome novel oxazine substituted 9-anilinoacridines have been synthesized, characterized and screened for in vitro antioxidant and anticancer activity. The docking studies were performed against topoisomerase II. The compounds 5a, 5h, 5i, 5j have significant antioxidant and anticancer activity.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Novel oxazine substituted 9-anilinoacridine derivatives have been synthesized. ► The compounds were characterized and screened for in vitro antioxidant activity. ► The anticancer activity of the compounds was also studied in DLA cell line. ► Docking studies were performed towards Topoisomerase II by Schrodinger software. ► The compounds 5a, 5h, 5i, 5j have significant antioxidant and anticancer activity.