Synthesis of novel fluorinated 1,5-benzothiazepine derivatives and their biological evaluation as anticancer and antibacterial agents

Abstract

A series of novel fluorinated 1,5-benzothiazepine derivatives were synthesized, characterized and evaluated for in vitro anticancer and antibacterial activity. The in vitro anticancer activity of the synthesized compounds 4a–h was evaluated against four human cancer cell lines namely lung (A549), breast (MCF-7), liver (HEPG2) and prostate (PC-3). Compounds 4c, 4d, 4g and 4h exhibited good activity with GI50 <10 µg ml-1 against all four human cancer cell lines which was comparable to standard drug adriamycin. Additionally, antibacterial activity of synthesized compounds was estimated using Resazurin Microtiter Assay (REMA) and compared with standard drug ampicillin. Among the synthesized compounds, 4c, 4d, 4g and 4h showed good antibacterial activity and all the synthesized compounds were found to be more active towards gram negative than gram positive bacteria. These promising results obtained from in vitro anticancer and antibacterial activity, inferred that the synthesized compounds are capable of being anticancer as well as antibacterial agents.