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Synthesis and Study of Medicinally Important Molecules

药用重要分子的合成与研究

基本信息

批准号：
10620871
负责人：
Mingji Dai
金额：
$ 42.21万
依托单位：
EMORY UNIVERSITY
依托单位国家：
美国
项目类别：
财政年份：
2018
资助国家：
美国
起止时间：
2018-08-04 至 2028-07-31
项目状态：
未结题

项目摘要

Project Summary/Abstract The goal of our research program is to innovate the strategy and methodology of organic synthesis and use these innovations to solve problems of biological and medicinal importance and ultimately impact human health. Our program focuses on the synthesis and study of both natural and unnatural molecules with potential for the treatment of cancer, neurological disorders, and drug resistant infectious diseases. We view the completion of a chemical synthesis as the beginning of a larger and deeper scholarly inquiry. It would enable us to profile the biology of the selected natural products and rationally designed small molecules, decipher their mechanism of actions, and optimize the lead compounds into biological probes and novel therapeutics. The selected terpenoid and alkaloid natural products represent both the state-of-the-art challenges for complex molecule synthesis as well as promising lead compounds for novel therapeutic development. Their structural complexity, natural scarcity, and unknown mechanism of actions have significantly hampered their biomedical development. We aim to fill this gap and move these molecules forward in the drug discovery pipeline with a multi-faceted approach centered on innovative chemical synthesis. The expected outcomes of this research will provide (i) new reactions and strategies in the toolbox of both medicinal chemists and synthetic chemists to prepare functional molecules, (ii) a reliable access to the selected target molecules with therapeutic importance, (iii) a collection of medicinally relevant molecules featuring structural novelty, complexity, and diversity for further and larger biological evaluations in academic institutions and pharmaceutical industries, and (iv) novel anticancer, anti-neurodegenerative and antimicrobial lead compounds with potentially novel mode of actions for in vivo and clinical evaluations.

项目摘要/摘要我们的研究计划的目标是创新有机合成和使用的策略和方法这些创新解决了生物和医学上的重要问题，并最终影响了人类健康。我们的计划重点是合成和研究具有潜力的天然和非天然分子。用于治疗癌症、神经疾病和抗药性传染病。我们查看完成一项化学合成，作为更大和更深入的学术探索的开始。它将使美国将对选定的天然产品的生物学进行描述，并合理设计小分子，破译它们的作用机理，并将先导化合物优化为生物探针和新的治疗药物。这个精选的萜类和生物碱天然产物代表了复合体的最新挑战分子合成以及有望用于新的治疗开发的先导化合物。他们的结构复杂性、自然稀缺性和未知的作用机制严重阻碍了它们的生物医学发展。我们的目标是填补这一空白，并通过一种以创新化学合成为中心的多方面方法。这项研究的预期结果将提供(I)药物化学家和合成化学家工具箱中的新反应和策略，以制备功能分子，(Ii)用治疗性方法可靠地接近选定的靶分子重要性，(Iii)具有结构新颖性、复杂性和医学上相关的分子的集合在学术机构和制药行业进行进一步和更大规模的生物评估的多样性，和(Iv)新型抗癌、抗神经退行性变和抗微生物先导化合物，具有潜在的新型体内和临床评价的作用模式。