Síntese e caracterização de complexos de paládio(II) com ligantes derivados de benzotiazol com potencial atividade antitumoral

Abstract

The discovery of the antitumor properties of cisplatin was extremely important for the treatment of cancer, such as testicular and ovarian cancer, and is considered one of the greatest accidental discoveries of modern science. This fact boosted research in search of new complexes that possess antitumor activity and that could act as metallopharmaceuticals. Benzothiazole stones show promise as they present a wide spectrum of biological activities already reported in the literature, such as antibacterial, antifungal, antitubercular and antitumor. This work aimed to synthesize and characterize three complexes based on palladium(II) with ligands derived from benzothiazole of the type [PdCl2(L)(PPh3)], where L is N-(benzothiazol-2-yl)acetamide (L1), N-(benzothiazol-2-yl)cyclopropanecarboxamide (L2) and N-(benzothiazol-2-yl)butyramide (L3) and subsequent evaluation of antitumor activity. The synthesized compounds were characterized by elemental analysis, absorption spectroscopy in the infrared region, 1H, 13C, 31P nuclear magnetic resonance, mass spectrometry and, in addition, two complexes were characterized by single-crystal X-ray diffraction. After characterization, it was possible to confirm the structure of the compounds and then evaluate the cellular solution of the complexes. The antitumor activity assays of the complexes were carried out against the ovarian cancer line and the complex [PdCl2(L)(PPh3)] showed promising results (IC50 = 1.51 μM), made from cisplatin. Therefore, the synthesized complexes demonstrate potential for future studies.