CAS: 13820-91-2; Potassium Amminetrichloroplatinate(Ii)

盐酸,Potassium Hexachloropalatinate(Iv),顺铂,铂置于ammonium Hydroxide体系中,用 水 用作溶剂,以126.70 G的收率获得三氯氨络铂(II)酸钾
参考文献:位阻含氟铂(II)配合物的合成,表征及生物活性
标题:位阻含氟铂(II)配合物的合成,表征及生物活性
摘要:摘要 吡铂是一种位阻抗肿瘤化合物,具有独特的化学和dna结合特性,但其疗效不如其他铂类药物.因此,通过在吡啶基团的2位引入氟原子和不同的离去基团配体,合成并表征了一系列位阻含氟铂(II)配合物y1-Y5 .已针对 A549,Mcf-7,Sw480,Hct116,Hepg2 人类癌细胞系和 Lo2 正常细胞对这些复合物进行了体外抗增殖活性评估.结果表明,Y1以2-氟吡啶配位和氯离子为离去基团的化合物在测试的癌细胞系中表现出更强的抗增殖活性和选择性,尤其是对a549癌细胞.通过紫外吸收和荧光滴定测定dna结合常数,Y1与dna的结合能力远强于其他化合物,这表明y1具有更好的dna损伤能力.复合物对细胞凋亡的测定,结果与mtt法一致,Y1细胞凋亡率达到38.9%.因此,我们的工作为开发新型铂基抗肿瘤药物提供了一种有利的方法.
Doi:10.1080/00958972.2023.2219820

专利信息

专利号:US-7238823-B2
优先权日:2005-06-30
标 题 :Platinum complexes with mononitrile-containing ligands
发明人：XIAO ZEJUN; HAUSHEER FREDERICK H; PETLURU PAVANKUMAR
权利人:BIONUMERIK PHARMACEUTICALS INC
摘要:Disclosed herein are novel platinum-based complexes possessing one nitrile substituent group (mononitrile) covalently-bonded to the platinum, one or more nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA and leaving groups (i.e., L 1 and L 2 ) which can be hydrolyzed in vivo to active species, which can then form coordinate adducts with DNA or RNA at the Guanine or Adenine bases thereof. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as methods of treatment of various types of cancer by the administration of a pharmaceutically-effective dose of said novel platinum complexes.

专利号:US-7569606-B2
优先权日:2006-01-26
标 题 :Platinum complexes with mononitrile-containing ligands
发明人：XIAO ZEJUN; HAUSHEER FREDERICK H; PETLURU PAVANKUMAR
权利人:BIONUMERIK PHARMACEUTICALS INC
摘要:Disclosed herein are novel platinum-based complexes possessing one nitrile substituent group (mononitrile) covalently-bonded to the platinum, one or more nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA and leaving groups (i.e., L 1 and L 2 )which can be hydrolyzed iii vivo to active species, which can then form coordinate adducts with DNA or RNA at the Guanine or Adenine bases thereof. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as methods of treatment of various types of cancer by the administration of a pharmaceutically-effective dose of said novel platinum complexes.