SYNTHESIS OF TARGET SPECIFIC ANTICANCER AGENTS

提出了顺铂系列甾体缀合物的合成方法

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.