<em>In vitro</em> biological evaluation of novel N-substituted 2,4-dihydroxythiobenzamides

Abstract

As continuation of the studies on the synthesis and evaluation of biologically active compounds functionalized by 2,4-dihydroxyphenyl substituent, a series of N-modified thiobenzamides have been prepared. They have been obtained by the reaction of the corresponding amines with the electrophilic thioacylating agent. The compounds have been subjected to <em>in vitro</em> antifungal activity screening against phytopathogenic fungi and antiproliferative potency against human cancer cell lines. N-(2,1,3-Benzothiadiazol-5-yl)-2,4-dihydroxybenzothioamide exhibits the highest antifungal activity, especially against <em>R. solani</em> and <em>P. cactorum</em>. 2,4-Dihydroxy-N'-(3-methyl-1,3-benzothiazol-2(3<em>H</em>)-ilidene)benzothiohydrazide shows high antiproliferative potency against the SW707 cells at IC₅₀ = 2 &micro;M, similar to that of cisplatin. To explain differences in the activity of the compounds, their <em>in silico</em> properties have been estimated.