SYNTHESIS OF TARGET SPECIFIC ANTICANCER AGENTS

目标特异性抗癌剂的合成

• 批准号: 6296614
• 负责人: KEN LEE
• 金额: $ 13.14万
• 依托单位: JACKSON STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-01-01 至 1999-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6296614
• 关键词: antineoplastics; breast neoplasms; carboxylate; chemical addition; chemical conjugate; chemical structure function; cis platinum compound; drug delivery systems; drug design /synthesis /production; drug screening /evaluation; estradiol; hydropathy; neoplasm /cancer chemotherapy; pharmacokinetics; progesterone; steroid analog; steroid hormone receptor; testis neoplasms; testosterone

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.

提出了顺铂系列甾体缀合物的合成方法