Novel di-n-butyltin(IV) derivatives: Synthesis, high levels of cytotoxicity in tumor cells and the induction of apoptosis in KB cancer cells

Two classes of dibutyltin(IV) hydroxamates complexes, formulated as the mononuclear mixed-ligand diorganotin(IV) complex [nBu2Sn(HL)Cl] a and the tetranuclear [nBu4Sn2(HL)2(L)]2b were fully characterized. X-ray diffraction analyses were also carried out for the representative complexes [nBu2Sn(2,6-F2C6H3C(O)NHO)Cl](4a) and [[nBu4Sn2{3-BrC6H4C(O)NHO}2{3-BrC6H4C(NO)O}]2](1b). The cytotoxicity of all compounds was tested by MTT and SRB assays against three human tumor cell lines HL-60, BGC-823 and KB. 1b and 4a have been shown to be more potent antitumor agents than other compounds and cisplatin. Annexin V FITC-PI assay was consistent with the MTT results. Cell cycle assay results indicated that KB cells displayed an arrest in the G0/G1 phase and a decrease of S phase of the cell cycle at the low concentrations of 1b, 4a.

Two classes of dibutyltin(IV) hydroxamates complexes were prepared and evaluated for in vitro antitumor activities. Annexin V FITC-PI assay and cell cycle assay was consistent with the MTT results. Figure optionsDownload as PowerPoint slideHighlights
► Two novel diorganotin(IV) complexes as anticancer agents.
► High levels antitumor activity against HL-60, BGC-823 and KB in vitro.
► Induces apoptosis in KB cancer cells at the low concentrations.