title: Monofunctional platinum complexes showing potent cytotoxicity against human liver carcinoma cell line BEL-7402.
abstract: Three novel Pt(II) complexes [PtL(1)'Cl] I (L(1)' = glycine-N'-8-quinolylamide), [PtL(2)'Cl] II (L(2)' = l-alanine-N'-8-quinolylamide), and [PtL(3)Cl] III [L(3) = N-(tert-butoxycarbonyl)-l-methionine-N'-8-quinolylamide] have been synthesized and characterized. The crystal structure of complexes II and III showed that the ligands are three-coordinated with only one Cl(-) as the leaving group. Complex II crystallized in the monoclinic system with space group P2(1), a = 9.502(2) A, b = 4.724(1) A, c = 14.800(3) A, while complex III crystallized in the orthorhombic system with space group P2(1)2(1)2(1), a = 5.441(1) A, b = 12.978(3) A, c = 29.438(6) A. These complexes have been tested against a wide range of tumor cell lines including BEL-7402, HCT-116, SPC-A4, MOLT-4, P388, HL-60, A-549, SGC-7901, MKN-28, and HO-8910. Complex III is highly cytotoxic against the HCT-116 (IC(50) = 0.38 microM), SPC-A4 (IC(50) = 0.43 microM), BEL-7402 (IC(50) = 0.43 microM), and MOLT-4 (IC(50) = 0.61 microM) cell lines. The cell line most sensitive to III is human liver carcinoma cell line BEL-7402, which has a response rate of 75.1% at 6.6 x 10(-7) M, nearly 6 times higher than that of cisplatin.
authors.affiliation: State Key Laboratory of Coordination Chemistry, Coordination Chemistry Institute, Nanjing University, Nanjing 210093, P. R. China.
authors.forename: Junyong
authors.initials: J
authors.lastname: Zhang
authors.forename: Xiaoyong
authors.initials: X
authors.lastname: Wang
authors.forename: Chao
authors.initials: C
authors.lastname: Tu
authors.forename: Jun
authors.initials: J
authors.lastname: Lin
authors.forename: Jian
authors.initials: J
authors.lastname: Ding
authors.forename: Liping
authors.initials: L
authors.lastname: Lin
authors.forename: Zheming
authors.initials: Z
authors.lastname: Wang
authors.forename: Cheng
authors.initials: C
authors.lastname: He
authors.forename: Chunhua
authors.initials: C
authors.lastname: Yan
authors.forename: Xiaozeng
authors.initials: X
authors.lastname: You
authors.forename: Zijian
authors.initials: Z
authors.lastname: Guo
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008113:Liver Neoplasms; D008715:Methionine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C476599:chlorotris(N-(tert-butoxycarbonyl)methionine-N'-8-quinolylamide)platinum(II); D008715:Methionine