title: A nine-coordinated bismuth(III) complex derived from pentadentate 2,6-diacetylpyridine bis((4)N-methylthiosemicarbazone): crystal structure and both in vitro and in vivo biological evaluation.
abstract: Up to now, bismuth(III) complexes with thiosemicarbazones have been comparatively rare. Few in vivo biological studies have been carried out in comparison to the plentiful in vitro data. Here, an interesting nine-coordinated bismuth(III) complex, [Bi(H2L)(NO3)2]NO3 [1; H2L = 2,6-diacetylpyridine bis((4)N-methylthiosemicarbazone)], has been synthesized and structurally characterized. The analytical data reveal the formation of 1:1 (metal/ligand) stoichiometry. In vitro biological studies have indicated that the bismuth complex 1 has shown much higher antibacterial and anticancer activities than its parent ligand, especially with MIC = 10.66 μM against Bacillus cereus and Salmonella typhimurium and IC50 = 26.8 μM against K562 leukemia cells, respectively. More importantly, it also evidently inhibits H22 xenograft tumor growth on tumor-bearing mice (10 mg/kg; inhibitory rate = 61.6%). These results indicate that coordination to bismuth(III) might be an interesting strategy in the discovery of new anticancer drug candidates.
authors.affiliation: Polyoxometalates Chemistry Key Laboratory of Henan Province, Institute of Molecular and Crystal Engineering, College of Chemistry and Chemical Engineering, Henan University , Kaifeng 475004, People's Republic of China.
authors.forename: Ming-Xue
authors.initials: MX
authors.lastname: Li
authors.forename: Min
authors.initials: M
authors.lastname: Yang
authors.forename: Jing-Yang
authors.initials: JY
authors.lastname: Niu
authors.forename: Li-Zhi
authors.initials: LZ
authors.lastname: Zhang
authors.forename: Song-Qiang
authors.initials: SQ
authors.lastname: Xie
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001409:Bacillus cereus / Q000187:drug effects*; D001729:Bismuth / Q000737:chemistry*; D049109:Cell Proliferation / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020014:K562 Cells; D008114:Liver Neoplasms, Experimental / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D012486:Salmonella typhimurium / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000737:chemistry*
chemical_list: C000591678:2,6-diacetylpyridine bis((4)N-methylthiosemicarbazone); D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D056831:Coordination Complexes; D013882:Thiosemicarbazones; D001729:Bismuth