Synthesis and Evaluation of Cytotoxic Activity of New Analogues of 4‐Substituted 1,2,4‐Benzothiadiazine‐1,1‐dioxide

Abstract

A new series of 4‐benzyl analogues of 1,2,4‐benzothiadiazine‐1,1‐dioxide was synthesized. All these compounds were subsequently tested for in vitro anti‐cancer activity against cancer cell lines selected by National Cancer Institute using one dose (10⁻⁵ M), following their standard screening procedure. The new compounds were characterized by ¹H NMR, ¹³C NMR, LCMS, and IR techniques. All the synthesized compounds showed sensitivity against tested cancer cell lines. Notably, the compound having 3‐fluoro‐4‐methoxybenzyl group on 1,2,4‐benzothiadiazine‐1,1‐dioxide ring exhibited the most promising cytotoxicity effect. It displayed a growth percentage oscillating between −32.82 % and 93.85 % on Melanoma and Breast cancer cell lines, respectively. Additionally, this compound demonstrated a significant antiproliferative effect on Leukaemia and CNS cancer cell lines. The most affected cell lines were MDA‐MB‐468 (Breast Cancer, lethality is 32.82 %) and MDA‐MB‐435 (Melanoma, −15.62 %). Other compounds in the series also demonstrated considerable antiproliferative effects on Breast cancer cell line.