Synthesis, characterization and antitumor activity of new type binuclear platinum(II) complexes

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal

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Author(s)

  • Jinchao Zhang
  • Lei Liu
  • Yuqiu Gong
  • Xiaoming Zheng
  • Jingrong Cui
  • Shigang Shen

Detail(s)

Original languageEnglish
Pages (from-to)2322-2327
Journal / PublicationEuropean Journal of Medicinal Chemistry
Volume44
Issue number5
Publication statusPublished - May 2009

Abstract

Five new type binuclear platinum(II) complexes (a-e) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, UV, 1H NMR and mass spectral techniques. The cytotoxicity of the complexes was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and sulforhodamine B (SRB) assays. The acute toxicity and antitumor activity of complex e in vivo were also studied. The results indicate that complexes a-d have no activity against HL-60, MCF-7, BGC-823, EJ and HCT-8 cell lines, with a higher IC50 value (>50 μM). Complex e confers substantially greater cytotoxicity against HL-60, MCF-7, BGC-823, EJ and HCT-8 cell lines with an IC50 value of 0.02 ± 0.009, 1.70 ± 0.21, 4.00 ± 0.35, 0.98 ± 0.02 and 1.02 ± 0.21 μM, respectively. LD50 of complex e is 815.3 mg/kg, it was significantly higher than that of cisplatin and carboplatin. Complex e at dose of 4, 12 and 20 mg/kg has no activity against mouse hepatocarcinoma H22 and Lewis lung carcinoma in mice, but displays significant activity against human ovarian carcinoma A2780 and human colon carcinoma HCT-116 in nude mice at dose of 12 mg/kg, and activity is similar to that of cisplatin at dose of 4 mg/kg. Complex e at dose of 20 mg/kg has no activity against human lung adenocarcinoma A549 in nude mice (P > 0.05). The results suggest that the species of amine for the new type binuclear platinum complexes have important effect on their cytotoxicity, and they may be a new class platinum anticancer drugs. © 2008 Elsevier Masson SAS. All rights reserved.

Research Area(s)

  • Acute toxicity, Binuclear platinum(II) complexes, Cytotoxicity, Synthesis

Citation Format(s)

Synthesis, characterization and antitumor activity of new type binuclear platinum(II) complexes. / Zhang, Jinchao; Liu, Lei; Gong, Yuqiu; Zheng, Xiaoming; Yang, Mengsu; Cui, Jingrong; Shen, Shigang.

In: European Journal of Medicinal Chemistry, Vol. 44, No. 5, 05.2009, p. 2322-2327.

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal