Tin thiocarbonohydrazone complexes: synthesis, crystal structures and biological evaluation

• Published in: Toxicology research (Cambridge) Vol. 8; no. 6; pp. 862 - 867
• Main Authors: Wang, Jin, Wang, Yu-Ting, Fang, Yan, Lu, Yan-Li, Li, Ming-Xue
• Format: Journal Article
• Language: English
• Published: England Royal Society of Chemistry 01.11.2019
• Subjects: Acute toxicity; Anticancer properties; Antitumor activity; Crystal structure; Crystallography; Cytotoxicity; Hepatocellular carcinoma; Hydroxybenzaldehydes; Infrared spectroscopy; Organotin; Selectivity; Toxicity
• ISSN: 2045-452X; 2045-4538; 2045-4538
• DOI: 10.1039/c9tx00109c

In this article, three organotin complexes formulated as [(Me) 2 Sn(H 2 L 1 )] ( 1 ), [(Ph) 2 Sn(H 2 L 1 )]·MeOH ( 2 ) and [(Me) 2 Sn(HL 2 )(OAc)] 4 (Me) 2 O ( 3 ) (H 4 L 1 = bis(2-hydroxybenzaldehyde) thiocarbohydrazone and H 2 L 2 = bis(2-acetylpyrazine) thiocarbonohydrazone) have been synthesized and structurally characterized. Growth inhibition assays indicated that both the proligands and the three complexes are capable of showing anticancer activity against the human hepatocellular carcinoma HepG2 cells with H 2 L 2 and complex 3 showing much higher cytotoxic potential. Subsequent toxicity studies on normal QSG7701cells showed that complex 3 has the highest tumor cell selectivity, and its IC 50 value on QSG7701 cells is 8.48 fold higher than that in HepG2 cells. In acute toxicity experiments, complex 3 produces a dose-dependent effect in NIH mice with a LD 50 value of 17.2 mg kg −1 . Three organotin thiocarbonohydrazone complexes have been synthesized, and growth inhibition assays indicated that complex 3 has the highest tumor cell selectivity.