SYNTHESIS OF TARGET SPECIFIC ANTICANCER AGENTS

目标特异性抗癌剂的合成

• 批准号: 6437015
• 负责人: KEN LEE
• 金额: $ 25.93万
• 依托单位: JACKSON STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-01-01 至 2002-01-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6437015
• 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.

提出合成顺铂系列甾体结合物 作为目标特异性抗癌药物。 雌二醇、睾酮和 黄体酮衍生物，可引导药物并释放 肿瘤器官选择顺铂用于乳腺和睾丸 具有类固醇受体的癌症。 类固醇之间的结合 西铂是利用羧酸根基团结合铂 金属井。 这种羧酸酯基团将被引入到16-、17-或 通过亲核加成反应得到相关类固醇的20位 与类固醇酮有关的酯。 合成的辛醇/磷酸盐缓冲液分配系数 将测量缀合的新试剂的亲脂性。 这 缀合物的抗肿瘤活性和其他药理活性 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。