公开(公告)号：KR100807358B1

公开(公告)日：2008-02-28

申请号：KR1020070038055

申请日：2007-04-18

Applicant: (주)씨앤팜

Inventor： 손연수 ,  유지영 ,  전용주

IPC: C07F17/02 ,  C07F9/06 ,  C07F9/02 ,  B82Y5/00

CPC classification number: C07F15/0093

Abstract: A cyclotriphosphazene-platinum(II) conjugate is provided to show high selectivity on a cancer tissue and excellent anticancer effect due to excellent permeation-retention property effect on the cancer tissue. A cyclotriphosphazene-platinum(II) conjugate is represented by the formula(1), where n is 7, 12 or 16; m is 0, 1 or 2; x is 1; each y and z is respectively 0 or 1; and each R, R' and R' is respectively selected from the group consisting of (CH3)2CH-, (CH3)2CHCH2-, (C2H5)(CH3)CH- and (C6H5)CH2-; and A and A' are independently an amine monodendate or A and A' may bound to each other to form a chelate type diamine didendate. An anticancer composition comprises the cyclotriphosphazene-platinum(II) conjugate as an effective ingredient. A method for preparing the conjugate comprises the steps of: (a) hydrolyzing a cyclotriphosphazene represented by the formula(3) to prepare an alkali metal salt or an alkali earth metal salt thereof represented by the formula(4); and (b) coupling the compound of the formula(4) to a (diamine) platinum(II) complex represented by the formula(5), where the n, m, x, y, z, R, R', R", A and A' are same as defined above; M is two alkali metal ions selected from the group consisting of potassium ion and sodium ion or Ba^2+; and L is one or two anion ligand(s) selected from the group consisting of sulfuric acid ion and nitric acid ion.

Abstract translation: 提供了一种环三磷腈 - 铂（II）缀合物，以显示对癌组织的高选择性，并且由于对癌组织的优异的渗透保留性效应而具有优异的抗癌作用。 环三磷腈 - 铂（II）缀合物由式（1）表示，其中n为7,12或16; m为0,1或2; x为1; 每个y和z分别为0或1; 并且每个R，R'和R'分别选自（CH 3）2 CH-，（CH 3）2 CHCH 2 - ，（C 2 H 5）（CH 3）CH-和（C 6 H 5）CH 2 - ; 并且A和A'独立地是单一单胺或A和A'可以彼此结合以形成螯合型二胺胺二酸酯。 抗癌组合物包含环三磷腈 - 铂（II）缀合物作为有效成分。 制备共轭物的方法包括以下步骤：（a）水解由式（3）表示的环三磷腈以制备由式（4）表示的碱金属盐或碱土金属盐; 和（b）将式（4）的化合物与由式（5）表示的（二胺）铂（II）络合物偶合，其中n，m，x，y，z，R，R'，R“ ，A和A'与上述相同; M是选自钾离子和钠离子或Ba 2+的两种碱金属离子; L是选自以下的一种或两种阴离子配体： 的硫酸离子和硝酸离子。