1,5-Benzosulfonamide anthracenedione analogues of mitoxantrone as antibacterial and anticancer agents

Abstract

The new 1,5-disubstituted 9,10 anthraquninone compounds have been synthesized and characterized by FT-IR, ¹H and ¹³C NMR, and mass spectrometry. Mass fragmentation pattern confirms the structure of the synthesized analogues. The synthesized compounds (B1-B5) have been found active against Hela (cervix carcinoma), prostate cancer and breast cancer cell lines in comparison to mitoxantrone. B2 screened out to be best. IC₅₀ value of B2 and mitoxantrone against Hela cell lines have been observed to be 17μg/mL and 2.5μg/mL respectively. DNA intercalation has been proposed as per cell cycle analysis of B2 on Hela cell lines which show major alteration in G0/G1 and S phase. The results are further supported by molecular docking study of (B1-B5) compounds and mitoxantrone with quadruplex terminals i-motif. The compounds have also been evaluated for antibacterial activities.