Cytotoxic effects of indium(III) complexes with 2-acetylpyridine-N(4)-ortho-fluorophenylthiosemicarbazone and their radioactive 114mIn analogues against human glioma cells

• Published in: Polyhedron Vol. 164; pp. 219 - 227
• Main Authors: Aguirre, Andrea R., Parrilha, Gabrieli L., Diniz, Renata, Ribeiro, Beatriz Cancelier, Santos, Raquel G. Dos, Beraldo, Heloisa
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 15.05.2019; Elsevier
• Subjects: Chemistry; Chemistry, Inorganic & Nuclear; Crystallography; Cytotoxicity; Glioblastoma Cells; Indium; Physical Sciences; Radiopharmaceuticals; Science & Technology; Thiosemicarbazones; Cytotoxicity; Indium; Radiopharmaceuticals; Glioblastoma Cells; Thiosemicarbazones; IN(III) COMPLEXES; LIGANDS; MOLECULAR-STRUCTURE; GALLIUM(III); 2-ACETYLPYRIDINE THIOSEMICARBAZONES; CRYSTAL; BINDING
• ISSN: 0277-5387; 1873-3719
• DOI: 10.1016/j.poly.2019.02.055

Complexes [In(2Ac4oFPh)Cl2(MeOH)] (1) and [In(2Ac4oFPh)Cl2] (2) were obtained with 2-acetylpyridine-N(4)-ortho-fluorophenyl thiosemicarbazone. Neutron activation of (1) and (2) resulted in the formation of the 114mIn/115mIn analogues (*1) and (*2). The non-radioactive and radioactive complexes showed similar cytotoxic effects and were as active as the parent thiosemicarbazone against U87 glioma cells. [Display omitted] Complexes [In(2Ac4oFPh)Cl2(MeOH)] (1) and [In(2Ac4oFPh)Cl2]·0.5EtOH (2) were obtained with 2-acetylpyridine-N(4)-ortho-fluorophenyl thiosemicarbazone (H2Ac4oFPh). Neutron activation of 1 and 2 resulted in the formation of the 114mIn/115mIn analogues (*1) and (*2). The thiosemicarbazone ligand, the non-radioactive and radioactive complexes were assayed for their cytotoxic effects against U87 human glioblastoma cells. While radioactive and non-radioactive InCl3 were devoid of cytotoxic activity, complexes (1) and (2) and their radioactive analogues (*1) and (*2) showed similar cytotoxic effects and were as active as the parent thiosemicarbazone against U87 glioma cells. Since the radioactive complexes revealed to keep the thiosemicarbazone cytotoxicity, if these complexes are produced with high specific activity, they might constitute an interesting platform for the development of prototype radiotracer drugs for treatment of glioma neoplasia by delivering high radiation dose to the tumor cells.