SYNTHESIS OF TARGET SPECIFIC ANTICANCER AGENTS

本文报道了一系列顺铂甾体偶联物的合成 作为靶向特异性抗癌剂。 雌二醇，睾酮， 孕酮衍生物，其可以引导药剂并递送 顺铂对肿瘤器官的作用选择乳腺和睾丸 具有类固醇受体的癌症。 甾体类化合物 而顺铂是利用羧酸根结合铂 金属好。 这种羧酸酯基团将被引入到16-、17-或18-羧基上。 20-通过亲核加成反应确定相关甾体的位置 与甾体酮有关的酯。 合成的正辛醇/磷酸盐缓冲液分配系数 将测量缀合的新试剂的亲脂性。 的 缀合物的抗肿瘤活性和其它药理活性 和甾体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.