Synthesis of Non-GMP Small Molecules

非 GMP 小分子的合成

• 批准号: 8177680
• 负责人: CHARLES KANE
• 金额: $ 10.6万
• 依托单位: STARKS ASSOCIATES, INC.
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-02-18 至 2012-07-12
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8177680
• 关键词: Antineoplastic Agents; Arts; Biological; Biological Factors; Chemicals; Chemistry; Contractor; Contracts; Development; Developmental Therapeutics Program; Division of Cancer Treatment and Diagnosis; Evaluation; Funding; Heterocyclic Steroids; Lead; Literature; Malignant Neoplasms; Methodology; Methods; Mission; Pharmacodynamics; Property; Recommendation; Series; Staging; United States National Institutes of Health; Work; abstracting; analog; chemical synthesis; drug development; improved; novel; programs; small molecule; steroid analog

Abstract: The addition of ARRA funds will be utilized for synthesis of the anticancer agent known in the literature; those can be further studied in the NCI¿s anticancer program. The mission of the Developmental Therapeutics Program (DTP) is the development of novel synthetic and characterized natural products as potential anti-cancer agents. Towards this mission the contract will be devoted to the synthesis of small molecules needed by the various programs of the Division of Cancer Treatment and Diagnosis (DCTD), and other NIH divisions. This contract will provide essential synthesis support for the early stages of the drug development program. The small molecules assigned for the syntheses encompass a variety of structural classes; e.g., carbocyclics, heterocyclics, steroid analogs, and natural products. They originate from the NExT initiative of the DCTD, Biological Evaluation Committee (BEC), and other NCI, and NIH programs. Under the scope of the these programs, the synthesis of a limited series of analogs in order to improve the potencies and pharmacodynamic properties of the lead compound, where the core chemistry is either well established or less documented, were also undertaken. The remaining 10% of the work has originated other NCI, NIH programs. The purity and identity of all resynthesized compounds and intermediates were established by state-of-the-art physico-chemical methods. The quantities synthesized would vary from 200 mg to 100 grams. The overall objective of the contract will be the ¿Non-GMP¿ chemical synthesis of compounds of good purity needed for the cancer NExT program, and compounds arising from recommendation of the Biological Evaluation Committee. The new contract will be utilized for the purpose of synthesis of active single compound leads and their analogs using parallel synthesis methodology, as sometimes required by the NCI programs.

抽象的： ARRA资金的添加将用于合成文献中已知的抗癌药。这些可以在NCIS抗癌计划中进一步研究。 发育治疗计划（DTP）的任务是开发新型合成和将天然产物作为潜在的抗癌剂的特征。为了实现这一任务，合同将致力于癌症治疗和诊断分区（DCTD）和其他NIH划分所需的小分子的综合。该合同将为药物开发计划的早期阶段提供基本的综合支持。为合成的小分子包括各种结构类别；例如，碳循环，杂环，类固醇类似物和天然产物。它们源自DCTD，生物评估委员会（BEC）和其他NCI和NIH计划的下一项计划。在这些程序的范围下，合成了一系列有限的类似物，以改善铅化合物的电位和药效学特性，在该化合物中，还进行了核心化学的确定性良好或记录在其中。其余10％的工作源于其他NCI，NIH计划。所有重新合成化合物和中间体的纯度和身份都是通过最先进的物理化学方法建立的。合成的数量将从200 mg到100克不等。合同的总体目的是``非GMP。癌症所需的良好纯度化合物的化学综合，并由生物评估委员会的建议引起的化合物。正如NCI程序有时所要求的那样，将使用新合同用于合成活跃的单个化合物铅及其类似物的目的。