Design, synthesis and biological evaluation of a novel series of glycosylated platinum(iv) complexes as antitumor agents. Issue 25 (2nd June 2016)

• Record Type: Journal Article
• Authors: Wang, Qingpeng; Huang, Zhonglv; Ma, Jing; Lu, Xiaolin; Zhang, Li; Wang, Xin; George Wang, Peng
• Is Part Of: Dalton transactions. Volume 45:Issue 25(2016)
• Page Start: 10366
• Page End: 10374
• Publication Date: 2016-06-02
• Subjects: Chemistry, Inorganic -- Periodicals; Chemistry, Physical and theoretical -- Periodicals; Chemistry, Inorganic -- Periodicals; 546.05
• DOI: 10.1039/c6dt01562j
• Languages: English
• ISSNs: 1477-9226

Abstract

Abstract : A new series of glycosylated Pt(iv ) complexes were designed, synthesized and evaluated for antitumor activities in vitro and in vivo . Abstract : A new series of glycosylated Pt(iv ) complexes were designed, synthesized and evaluated for antitumor activities in vitro and in vivo . The incorporation of glycosyl groups to the Pt(iv ) system has much influence on the antitumor abilities. Four lead compounds with activities comparable or even superior to cisplatin and oxaliplatin are screened out. These Pt(iv ) complexes could be reduced to release Pt(ii ) complexes and cause the death of tumour cells. The apoptosis-inducing properties of these compounds are similar to cisplatin. The accumulation of the glycosylated Pt(iv ) complexes in cells and DNA is higher than cisplatin and oxaliplatin. The in vivo assay demonstrates that the tested compounds inhibit the growth of HepG2 tumors with low toxicity.