The University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, England, UK.
Nat Commun. 2010 Sep 21;1:80. doi: 10.1038/ncomms1081.
Biologically active molecules can be identified through the screening of small-molecule libraries. Deficiencies in current compound collections are evidenced by the continuing decline in drug-discovery successes. Typically, such collections are comprised of large numbers of structurally similar compounds. A general consensus has emerged that library size is not everything; library diversity, in terms of molecular structure and thus function, is crucial. Diversity-oriented synthesis (DOS) aims to generate such structural diversity in an efficient manner. Recent years have witnessed significant achievements in the field, which help to validate the usefulness of DOS as a tool for the discovery of novel, biologically interesting small molecules.
生物活性分子可以通过筛选小分子文库来进行鉴定。目前化合物库的不足体现在药物发现成功率的持续下降上。通常，这些化合物库由大量结构相似的化合物组成。人们普遍认为，库的大小并不是唯一重要的因素；库的多样性，即分子结构，因此功能，是至关重要的。定向合成（DOS）旨在以有效的方式产生这种结构多样性。近年来，该领域取得了重大进展，这有助于验证 DOS 作为一种发现新型生物活性小分子的工具的有用性。
