Sanofi-Aventis Deutschland GmbH, R&D LGCR/Chemistry, Industriepark Höchst G838, 65926 Frankfurt am Main, Germany.
Nat Prod Rep. 2014 Jan;31(1):35-60. doi: 10.1039/c3np70058e.
Covering: up to March 2013. In addition to their prominent role in basic biological and chemical research, natural products are a rich source of commercial products for the pharmaceutical and other industries. Industrial natural product chemistry is of fundamental importance for successful product development, as the vast majority (ca. 80%) of commercial drugs derived from natural products require synthetic efforts, either to enable economical access to bulk material, and/or to optimize drug properties through structural modifications. This review aims to illustrate issues on the pathway from lead to product, and how they have been successfully addressed by modern natural product chemistry. It is focused on natural products of current relevance that are, or are intended to be, used as pharmaceuticals.
截至 2013 年 3 月。除了在基础生物和化学研究中扮演重要角色外,天然产物也是医药和其他行业商业产品的丰富来源。工业天然产物化学对于成功的产品开发至关重要,因为绝大多数(约 80%)来源于天然产物的商业药物需要通过合成手段来实现,无论是为了经济地获得大量材料,还是为了通过结构修饰来优化药物性质。本篇综述旨在举例说明从先导化合物到产品的途径中存在的问题,以及现代天然产物化学如何成功地解决这些问题。它重点关注当前具有相关性、或意图作为药物使用的天然产物。