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Synthesis and Cytotoxic Evaluation of Novel Platinum(Ⅱ) Complexes with C2-Asymmetric and C2-Symmetric Chiral Vicinal Diamines
  • ISSN号:1001-604X
  • 期刊名称:《中国化学:英文版》
  • 时间:0
  • 分类:O624[理学—有机化学;理学—化学] O614.826[理学—无机化学;理学—化学]
  • 作者机构:[1]Department of Natural Products Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China, [2]Department of Pharmacology, School of Pharmacy, Fudan University, Shanghai 201203, China, [3]Key Lab of Smart Drug Delivery, Ministry of Education & PLA, Fudan University, Shanghai 201203, China
  • 相关基金: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.
中文摘要:

有 C2 不对称、 C2 对称的 1,2 肼的一系列新铂(II ) 建筑群被设计并且由方便方法综合了作为关键步的导致的减少的联合,包含钐 diiodide。cytotoxicity 的结果证明那加重(R, R )-11a 并且(S, S )-11a, 有不对称的 1,2 肼的二新奇的铂(II ) 建筑群,对所有白血病房间线比 oxaliplatin 的展出了更多的有势力 cytotoxicity。有趣地,(R, R )-11a 并且(S, S )-11a 比 oxaliplatin 的对三根稳固的癌症房间线表明了更少的有势力活动,它显示这二混合物可以仅仅有选择地禁止白血病房间线。相反,(R, R )-15a 并且(S, S )-15a, 有对称的 1,2 肼的二铂(II ) 建筑群,到对对稳固的癌症房间的所有白血病房间线和更多的有势力活动的 oxaliplatin 的显示出的类似的 cytotoxicity 排队。进一步的流动 cytometry 数据显示了那(R, R )-11a 能显然在 G2/M 阶段逮捕白血病 K562 房间。

英文摘要:

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.

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期刊信息
  • 《中国化学:英文版》
  • 主管单位:
  • 主办单位:中国化学会
  • 主编:
  • 地址:上海市枫林路354号中科院上海有机化学研究所
  • 邮编:200032
  • 邮箱:
  • 电话:021-54925243
  • 国际标准刊号:ISSN:1001-604X
  • 国内统一刊号:ISSN:31-1547/O6
  • 邮发代号:4-646
  • 获奖情况:
  • 中国期刊方阵“双高”期刊
  • 国内外数据库收录:
  • 美国化学文摘(网络版),荷兰文摘与引文数据库,美国科学引文索引(扩展库),日本日本科学技术振兴机构数据库,英国英国皇家化学学会文摘
  • 被引量:175