Eskitis Institute, Griffith University, Brisbane, Queensland 4111, Australia.
Future Med Chem. 2012 Jun;4(9):1067-84. doi: 10.4155/fmc.12.55.
Natural products (NPs) have historically been a fertile source of new drugs for the pharmaceutical industry. However, this once-popular approach has waned considerably over the past two decades as the high-throughput screening of megalibraries comprised mainly of molecules with non-natural (synthetic) motifs has unfolded. Contemporary high-throughput screening libraries contain molecules compliant with physicochemical profiles considered essential for downstream development. Until recently, there was no strategy that aligned NP screening with the same physicochemical profiles. An approach based on Log P has addressed these concerns and, together with advances in isolation, afforded NP leads in timelines compatible with pure compound screening. Concomitant progress related to access of biological resources has provided long-awaited legal certainty to further facilitate NP drug discovery.
天然产物（NPs）一直是制药行业新药的丰富来源。然而，在过去的二十年中，随着主要由非天然（合成）结构组成的高通量筛选大规模文库的展开，这种曾经流行的方法已经大大减少。当代高通量筛选文库包含符合被认为对下游开发至关重要的物理化学特征的分子。直到最近，还没有一种策略可以将 NP 筛选与相同的物理化学特征结合起来。基于 Log P 的方法解决了这些问题，并且与分离技术的进步一起，在与纯化合物筛选兼容的时间范围内提供了 NP 先导化合物。与生物资源获取相关的同时进展为进一步促进 NP 药物发现提供了期待已久的法律确定性。
