New platinum(II) monochelate and biskelate complexes with thiazol-2/5-carbaldehyde ligands thiosemicarbazone and their antitumor activity

Currently, one of the public health problems with the highest incidence in the world and in our country is cancer. In our country, the mortality rate of this disease is high, identifying different types of cancer in women (cervix and breast) and in men (stomach, lung and prostate). Cisplatin, Pt(NH3)2Cl2, is the clinically used anticancer drug used in cancer chemotherapy. The application of this drug produces collateral effects. In previous research, we have shown that the heterocyclic derivative, X-pyridine-3-carbaldehyde thiosemicarbazone, inhibits the growth of human tumor cells: HuTu80 (adenocarcinoma of the duodenum), MCF-7 (adenocarcinoma of the breast) and M-14 (melanoma). amelanotic).
In this work we describe the synthesis, characterization using IR and NMR spectroscopic techniques and in vitro cytotoxic evaluation of new platinum(II) complexes with ligands derived from thiazol-2/5-carbaldehyde thiosemicarbazone against different human tumor cell lines.

One of the public health problems is cancer. This disease is generated by the multiplication of abnormal cells that spread to any part of the body. In 2020, worldwide, it has been identified that lung cancer is the type of cancer with the highest frequency of deaths (1.8 million) compared to other types of cancer (colorectal, liver, gastric, breast, among others). ). In Peru, in 2018, 66,627 cases of cancer were diagnosed, with 33,098 deaths, with breast cancer and lung cancer being the types of cancer recorded with the highest incidence. One of the treatments used for this disease is chemotherapy, where cisplatin [cis-Pt(NH3)2Cl2], an anticancer drug, is used at a concentration of 1 mg/mL intravenously in patients suffering from various types of cancer. However, the concentrations of cisplatin used produce side effects such as nausea, vomiting, diarrhea, stomach irritation, nephrotoxicity, neurotoxicity, among others. For this reason, it is of great interest to develop new compounds with potential antitumor activity in some type of cancer and that present low toxicity in normal cells. Knowing that some complexes of transition metals with thiosemicarbazone ligands containing heterocyclic fragments have anticancer activity, our research group wants to prepare new complexes of platinum(II) with ligands derived from X-thiazole-2-/5-carbaldehyde thiosemicarbazone ( X=3,4-di-FluorPh, 3-F-Ph, 5-CH3, 4-Cl-Ph, 2-pyrrolyl, 2-CH3-Ph, 2-diethylamino, 2-ortho-tolyl, 2,4- di-Chloro-Ph, 2-Br, 2-NH2, 2-piperidinyl, 4-CH3/2-(CF3Ph), 4-CH3/2-pyridinyl) and evaluate its cytotoxic activity.