Realisation of small molecule libraries based on frameworks distantly related to natural products†,Organic & Biomolecular Chemistry

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Realisation of small molecule libraries based on frameworks distantly related to natural products†
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2018-04-11 00:00:00 , DOI: 10.1039/c8ob00688a
Anthony Aimon _{1,

2,

3,

4} , George Karageorgis _{1,

2,

3,

4,

5} , Jacob Masters _{1,

2,

3,

4,

5} , Mark Dow _{1,

2,

3,

4} , Philip G. E. Craven _{1,

2,

3,

4} , Martin Ohsten _{6,

7,

8} , Anthony Willaume _{6,

7,

8} , Rémy Morgentin _{6,

7,

8} , Nicolas Ruiz-Llamas _{6,

7,

8} , Hugues Lemoine _{6,

7,

8} , Tuomo Kalliokoski _{9,

10,

11} , Andrew J. Eatherton _{4,

12,

13,

14,

15} , Daniel J. Foley _{1,

2,

3,

4,

5} , Stephen P. Marsden _{1,

2,

3,

4} , Adam Nelson _{1,

2,

3,

4,

5}

Affiliation

The availability of high-quality screening compounds is of paramount importance for the discovery of innovative new medicines. Natural product (NP) frameworks can inspire the design of productive compound libraries. Here, we describe the design and synthesis of four compound libraries based on scaffolds that have broad NP-like features, but that are only distantly related to specific NPs. The optimisation of syntheses of the scaffolds using [5 + 2] cycloaddition chemistry is detailed, together with methods to yield exemplar decorated screening compounds. In each case, a library was nominated for production, leading to a total of >2900 screening compounds that augmented the Joint European Compound Library of the European Lead Factory.

中文翻译：

基于与天然产物密切相关的框架实现小分子文库†

高质量筛选化合物的可用性对于发现创新的新药物至关重要。天然产物（NP）框架可以激发生产性化合物库的设计。在这里，我们描述基于支架的四个化合物库的设计和合成，这些支架具有广泛的类似NP的功能，但是与特定的NP距离遥远。详细介绍了使用[5 + 2]环加成化学优化支架合成的方法，以及产生示例性修饰筛选化合物的方法。在每种情况下，都提名了一个用于生产的库，从而产生了总数超过2900种的筛选化合物，从而增强了欧洲铅工厂的联合欧洲化合物库。

更新日期：2018-04-11

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