| 摘要 |
PURPOSE: An anticancer agent of polyphosphazene-platinum(II) conjugate having tumor selectivity and biodecomposability, and a preparation method thereof are provided. The anticancer agent has improved tumor selectivity and has less adverse side effect. Therefore, the treatment efficiency of cancer can be improved. CONSTITUTION: The anticancer agent of polyphosphazene-platinum(II) conjugate having tumor selectivity and biodecomposability is represented by the formula(1), wherein x is repeated number of polyethyleneglycol, 7, 12 or 16; y is 0, 1 or 2; z is mole content of polyethyleneglycol, 0.5 to 1.5; n is polymerization degree, 30 to 100; A-A is diamine; the diamine is selected from trans(±)-1,2-diaminocyclohexane, 2,2-dimethyl-1,3-propandiamine and ethylenediamine. The method for preparing anticancer agent of polyphosphazene-platinum(ii) conjugate of the formula(1) comprises the steps of: (a) sequentially reacting polydichlorophosphagen of the formula(3) with sodium salt of hydrophilic methoxy polyethyleneglycol of the formula(5) and hydrophobic dipeptide ester of the formula(6) to prepare bipolar polyphosphagen of the formula(7); and (b) hydrolysis of dipeptide ester of the compound of the formula(7) in alcohol solution with alkali, and reacting the hydrolysis product with platinum(II) conjugate of the formula(8) : (A-A)PtL.
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