SYNTHESIS OF TARGET SPECIFIC ANTICANCER AGENTS

提出了一系列顺铂类化合物的合成方法 作为靶向的特定抗癌药物。雌二醇、睾丸素和 黄体酮衍生物，这可能是先导和递送 顺铂对肿瘤器官的选择适用于乳腺和睾丸 有类固醇受体的癌症。类固醇的偶联作用 而顺铂则是用羧酸基结合铂 金属井。这种羧酸基将被引入16-、17-或 相关甾体的20位亲核加成反应 与类固醇中的酮相关的酯。 合成的正辛醇/磷酸盐缓冲液分配系数 将对新试剂的亲脂性进行测定。这个 结合物的抗肿瘤活性及其他药理活性 类固醇衍生物将在药学院进行测试， 佛罗里达农工大学，塔拉哈西。

Synthesis of series of steroidal conjugates of cisplatin is proposed as target specific anti-cancer agents. Estradiol, testosterone, and progesterone derivatives, which may lead the agents and deliver cisplatin to the tumor organ are chose for breast and testicular cancers having steroidal receptors. The conjugation between steroid and ciplatin is to use the carboxylate group binding the platinum metal well. Such carboxylate group will be introduced to 16-, 17- or 20-position of related steroids by nucleophilic addition reaction of related ester with ketone of steroids. The octanol/phosphate buffer partition coefficients of synthesized conjugated will be measured for the lipophilicity of new agents. The anti-tumor activity and other pharmacological activity of conjugates and steroidal derivatives will be tested at School of Pharmacy, Florida A&M University, Tallahassee.