SYNTHESIS OF STABLE ISOTOPE-LABELED STEROIDS FOR THE MEASUREMENT OF ENDOGENOUS S

用于内源性 S 测量的稳定同位素标记类固醇的合成

• 批准号: 7976629
• 负责人: SCOTT LANDVATTER
• 金额: $ 71万
• 依托单位: ISOSCIENCES, LLC
• 依托单位国家: 美国
• 财政年份: 2009
• 资助国家: 美国
• 起止时间: 2009-03-01 至 2011-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7976629
• 关键词: SYNTHESIS; STABLE; ISOTOPE; LABELED; STEROIDS

This SBIR Phase II proposal elaborates on the success achieved during Phase I where IsoSciences was successful in developing synthetic methods for 1) The regioselective preparation of 2 and 4-methoxy-[13C,2H3] labeled estrogens and 2) The preparation of testosterone-[1,2,3-13C3]. The methodology developed in Phase I will be scaled up in Phase II such that IsoSciences, LLC will produce 100mg quantities of several stable-isotope labeled key steroid hormones including 2-, 3-, and 4-methoxyestrogens, estriol, testosterone, estrone, estradiol, and androstenedione and dehydroepiandrosterone. The selected compounds are believed to play critical roles in various cancers and thus have the potential to serve as cancer biomarkers. A significant stumbling block in the research area has been the lack of availability of stable isotope labeled standards for use in detecting and quantifying these key steroids. This Phase II contract will address that significant problem.

该SBIR II期提案详细阐述了在I期期间取得的成功，其中IsoSciences成功开发了1）2和4-甲氧基-[13 C，2 H3]标记雌激素的区域选择性制备和2）睾酮-[1，2，3 - 13 C3]的制备的合成方法。 在第一阶段开发的方法将在第二阶段扩大规模，以便IsoSciences，LLC将生产100毫克数量的几种稳定同位素标记的关键类固醇激素，包括2-，3-和4-甲氧基雌激素，雌三醇，睾酮，雌酮，雌二醇，雄烯二酮和脱氢表雄酮。所选择的化合物被认为在各种癌症中发挥关键作用，因此有可能作为癌症生物标志物。研究领域的一个重要障碍是缺乏用于检测和定量这些关键类固醇的稳定同位素标记标准品。第二阶段合同将解决这一重大问题。