Isothiocoumarin-3-carboxylic acid derivatives: Synthesis, anticancer and antitrypanosomal activity evaluation

• Isothiocoumarin-3-carboxylic acid derivatives synthesis based on 5-ylidenerhodanines.
• 4-Phenylthiazol-2-yl-amide (30) showed prominent anticancer activity (GI50 ≈ 1.5 μM).
• Synthesized compounds didn't exhibit significant antitrypanosomal (Tbb) effects.

A series of new isothiocoumarin-3-carboxylic acids derivatives had been obtained based on the 5-arylidenerhodanines hydrolysis. Anticancer activity screening allowed identification of 7,8-dimethoxy-1-oxo-1H-isothiochromene-3-carboxylic acid (4-phenylthiazol-2-yl)-amide (30) with the highest level of antimitotic activity (GI50NCI-H322M/NSC Lung Cancer = 1.28 μM). Evaluation of the antitrypanosomal activity against Trypanosoma brucei brucei showed that investigated compounds did not exhibit significant antiparasitic effects. Additionally, the most pharmacologically attractive compounds were non-toxic and well tolerated by the experimental animals.

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