Mixture-Based Synthetic Combinatorial Libraries
Mixture-Based Synthetic Combinatorial Libraries
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基于混合物的合成组合文库
DOI：
10.1002/chin.199949239
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发表时间：
1999
期刊：
影响因子：
--
通讯作者：
J. Ostresh
中科院分区：
文献类型：
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作者：
R. Houghten;C. Pinilla;J. Appel;S. Blondelle;C. Dooley;J. Eichler;A. Nefzi;J. Ostresh
自第一次描述以来的15年里，涵盖组合化学的概念和技术方法几乎在所有科学学科中都得到了广泛的接受。已经发表了1000多篇关于这个主题的文章，包括大量的书籍和期刊，每年都会举行一系列的“组合化学”研讨会。此外，还推出了关于这一主题的大学课程，并提供了互联网网站(www.5Z。Com是最完整的网站之一)。《科学》杂志承认组合化学是1998年科学研究的九项突破之一，最近提出了一个关于这一不断增长的领域历史的独特视角。2这一视角的重点将放在组合化学的力量上，更具体地说，是基于混合物的库，以加速基础研究和药物发现的化学信息获取。虽然已经提出了一些创新的方法，但大多数组合化学程序仍然倾向于通过使用Solidor溶液相法的并行合成方法来制备大量单独的化合物，这种方法经过了时间考验，但速度慢且成本高。相比之下，由化合物混合物组成的组合文库的合成和筛选是最早提出的组合方法之一，但仍未得到充分利用，经常受到怀疑。这一观点说明了基于混合的
In the 15 years since their first description, the conceptual and technical approaches that encompass combinatorial chemistry have gained wide acceptance across virtually all scientific disciplines. More than 1000 articles have been published on the subject, including numerous books and journals, and a range of “combichem” symposia are held each year. Also, college courses have been introduced on the subject, and Internet sites are available (www. 5z. com is one of the most complete). The journal Science recognized combinatorial chemistry as one of nine breakthroughs in scientific research for 1998, 1 and a unique perspective on the history of this growing field was recently presented. 2The emphasis in this Perspective will be on the power of combinatorial chemistry, more specifically mixturebased libraries, to accelerate chemical information acquisition for basic research and drug discovery. While a number of innovative approaches have been presented, the majority of combinatorial chemistry programs still prefer the time-tested but slow and expensive preparation of large numbers of individual compounds by parallel synthesis methods using either solidor solution-phase approaches. In contrast, the synthesis and screening of combinatorial libraries made up of mixtures of compounds, which was one of the first combinatorial approaches presented, is still underutilized and often regarded with skepticism. This Perspective illustrates the inherent strengths of mixture-based