Synthesis and in vitro cytotoxicity of novel hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes

Haibin Zhu; Kai Cui; Lianhong Wang; Shaohua Gou

doi:10.1016/j.bmcl.2005.08.025

Synthesis and in vitro cytotoxicity of novel hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes

Bioorg Med Chem Lett. 2005 Nov 15;15(22):4936-43. doi: 10.1016/j.bmcl.2005.08.025.

Authors

Haibin Zhu¹, Kai Cui, Lianhong Wang, Shaohua Gou

Affiliation

¹ State Key Laboratory of Coordination Chemistry, Nanjing University, Nanjing 210093, China.

PMID: 16169720
DOI: 10.1016/j.bmcl.2005.08.025

Abstract

Twenty-six new hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes having a seven-membered ring structure between a bidentate carrier ligand and a platinum atom have been synthesized and most of them were evaluated for their in vitro cytotoxicity toward A549 human non-small cell lung carcinoma and HCT-116 human colon cancer cell lines. The cytotoxicities of platinum complexes are related to the nature of the carrier ligand and leaving group. Complex 5'b, viz. cis-dichloro[(2R)-ethoxy-1,4-butanediamine] platinum (II), exhibits the greatest potency among those 21 tested platinum complexes in both cell lines.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amines / chemical synthesis*
Amines / chemistry
Amines / toxicity*
Cell Line, Tumor
Cell Proliferation / drug effects
Humans
Hydrophobic and Hydrophilic Interactions
Inhibitory Concentration 50
Molecular Structure
Organoplatinum Compounds / chemical synthesis*
Organoplatinum Compounds / chemistry
Organoplatinum Compounds / toxicity*
Structure-Activity Relationship

Substances

Amines
Organoplatinum Compounds