Chemical Biology Platform, Broad Institute of MIT and Harvard, 7 Cambridge Center, Cambridge, MA 02142, USA.
Curr Opin Chem Biol. 2010 Jun;14(3):362-70. doi: 10.1016/j.cbpa.2010.03.018. Epub 2010 Apr 19.
Compounds accessed through diversity-oriented synthesis (DOS) are showing promise in modulating the activities of several targets that are currently considered 'undruggable'. Recently many new DOS pathways have been developed employing multi-component reactions, cycloadditions, ring-closing metathesis and tandem processes. Functional group pairing and 'build/couple/pair' strategies have been described as a means for generating structural diversity. Efforts have also been directed towards developing DOS libraries based on privileged scaffolds. Recent studies have provided several compelling examples for the utility of DOS compounds for producing novel biological probes and application of DOS in the context of drug discovery is extremely appealing.
通过多样性导向合成（DOS）获得的化合物在调节几个目前被认为“不可成药”的靶点的活性方面显示出了前景。最近，已经开发了许多新的 DOS 途径，采用多组分反应、环加成、环 closing metathesis 和串联过程。官能团配对和“构建/偶联/配对”策略被描述为产生结构多样性的一种手段。人们还致力于开发基于特权支架的 DOS 文库。最近的研究为 DOS 化合物在产生新型生物探针方面的应用提供了几个令人信服的例子，DOS 在药物发现中的应用也极具吸引力。
