铂类抗癌配合物构效关系的理论探讨

A Theoretical Discusslon on the Structure-Activity Relationship of Anticancer Platinum Complexes

基于铂抗癌配合物在体内的历程和化学反应探讨了它们的结构和活性之间的关系，获得决定抗癌活性大小的主要因素，包括配合物分子的脂溶性和空间体积、构型、离去基团的反应性以及载体基团的特性。提出了铂配合物具有较高抗癌活性的结构要求①非离子型②小的空间体积③顺式构型④含脂溶性的氨（胺）载体和以Ｃｌ￣（－）或二元羧酸作离去基团。

Based on the moving path and chemical reactions of platinum anticancer complexes in vivo,their structure-activity relationship was dis-cussed and the major chemical parameters in the determination of the activity were obtained.These parameters include the lipophilic ability and steric size of the complex molecules,configuration,the activity of leaving groups and nature of carrier group.It is proposed that the complex with high anticancer activity should meet the following requirements:(1)no-nionic species;(2)small steric size;(3)cis-configuration;(4)containing lipophilic amine carrier of small size and Cl￣(-) or bicarboxylato as the lea- ving group.