Synthesis of Non-GMP Small Molecules

非 GMP 小分子的合成

• 批准号: 8328348
• 负责人: MARY TANGA
• 金额: $ 10万
• 依托单位: SRI INTERNATIONAL
• 依托单位国家: 美国
• 财政年份: 2006
• 资助国家: 美国
• 起止时间: 2006-09-29 至 2012-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8328348
• 关键词: Antineoplastic Agents; Biological; Biological Factors; Chemicals; Chemistry; 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; analog; cancer diagnosis; cancer therapy; chemical synthesis; drug development; improved; novel; programs; small molecule; steroid analog

The addition of ARRA funds will be utilized for synthesis and acquisition 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.

ARRA资金的增加将用于合成和收购文献中已知的抗癌药物；这些可以在 NCI 的抗癌项目中得到进一步研究。 发展治疗计划 (DTP) 的使命是开发新型合成和表征的天然产品作为潜在的抗癌药物。为了实现这一使命，该合同将致力于合成癌症治疗和诊断部门 (DCTD) 以及其他 NIH 部门的各种项目所需的小分子。该合同将为药物开发计划的早期阶段提供必要的合成支持。用于合成的小分子涵盖多种结构类别；例如，碳环、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) 以及其他 NCI 和 NIH 项目的 NExT 倡议。在这些计划的范围内，还进行了有限系列类似物的合成，以提高先导化合物的效力和药效学特性，其中核心化学要么已充分确立，要么记录较少。其余 10% 的工作源自其他 NCI、NIH 项目。所有重新合成的化合物和中间体的纯度和特性均通过最先进的物理化学方法确定。合成量从 200 毫克到 100 克不等。该合同的总体目标是“非 GMP”化学合成癌症 NExT 计划所需的高纯度化合物，以及生物评估委员会推荐的化合物。新合同将用于使用平行合成方法合成活性单一先导化合物及其类似物，这有时是 NCI 项目所要求的。