摘要
A series of new platinum（II） complexes with C2-asymmetric and C2-symmetric 1,2-diamines were designed and synthesized by convenient methods, involving samarium diiodide induced reductive coupling as the key step. The results of cytotoxicity showed that compounds （R,R）-lla and （S,S）-lla, two novel platinum（II） complexes with asymmetric 1,2-diamines, exhibited more potent cytotoxicity than that of oxaliplatin against all leukemia cell lines. Interestingly, （R,R）-lla and （S,S）-lla demonstrated less potent activity against three solid cancer cell lines than that of oxaliplatin, which indicated that these two compounds may only selectively inhibit the leukemia cell lines. In contrast, （R,R）-ISa and （S,S）-15a, two platinum（II） complexes with symmetric 1,2-diamines, showed similar cyto- toxicity to that of oxaliplatin against all leukemia cell lines and more potent activity against solid cancer cell lines. Further flow cytometry data indicated that （R,R）-lla could obviously arrest leukemia K562 cells in G2/M phases.
A series of new platinum（II） complexes with C2-asymmetric and C2-symmetric 1,2-diamines were designed and synthesized by convenient methods, involving samarium diiodide induced reductive coupling as the key step. The results of cytotoxicity showed that compounds （R,R）-lla and （S,S）-lla, two novel platinum（II） complexes with asymmetric 1,2-diamines, exhibited more potent cytotoxicity than that of oxaliplatin against all leukemia cell lines. Interestingly, （R,R）-lla and （S,S）-lla demonstrated less potent activity against three solid cancer cell lines than that of oxaliplatin, which indicated that these two compounds may only selectively inhibit the leukemia cell lines. In contrast, （R,R）-ISa and （S,S）-15a, two platinum（II） complexes with symmetric 1,2-diamines, showed similar cyto- toxicity to that of oxaliplatin against all leukemia cell lines and more potent activity against solid cancer cell lines. Further flow cytometry data indicated that （R,R）-lla could obviously arrest leukemia K562 cells in G2/M phases.
基金
Acknowledgement Financial support by the National Natural Science Foundation of China （No. 81172920）, the Shanghai Municipal Committee of Science and Technology （No. 10431903100）, and the National Basic Research Pro- gram of China （973 Program, No. 2010CB912603） are acknowledged. We would like to thank Prof. G.-Q. Lin for the guidance of asymmetric synthesis.
