Synthesis of Novel Platinum(II) Complexes with Acylthiourea-Derived Organic Quenchants and Evaluation of Antitumor Activity in Mouse TA3 Mammary Adenocarcinoma Cells
Keywords:
Platinum(II) complexes, Acylthiourea, Cytotoxic/antitumor activity, Cell growthAbstract
One of the areas of bioinorganic chemistry that has had a great development in the last years is the use of coordination compounds for medical purposes. Thus, evidence exists that thiourea derivative ligands, R1NH-CS-NHR2, and their platinum(II) complexes act as antitumor agents. The present work inform about the synthesis and characterization of acylthiourea ligands (HL), PhCONH-CS-NR2 and the respective platinum(II) complexes, cis- PtL2 [ R = diphenylamine and morpholyne], and the evaluation of the biological activity against the mouse TA3 mammary adenocarcinoma cell line. The molecular structures of the synthesized platinum(II) complexes show a nearly square-planar geometry with two deprotonated ligands (L) coordinated to the metal through the oxygen and sulfur atoms in a cis configuration. The antitumor activity of the platinum(II) complexes with acylthiourea ligands was evaluated in vitro against the mouse TA3 mammary adenocarcinoma cell line. The studied complexes exhibited much higher cytotoxic activity than their respective ligands, being the cis-bis(N-morpholyn-N´-benzoylthioureato) platinum(II) complex, [Pt(L2)2], the one that showed a high cytotoxic activity at low micromolar concentrations (IC50 = 0.98 μM). This result indicated that the bounding of the ligands to metallic center increases its antitumor activity.
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