Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai 400076, India.
Org Biomol Chem. 2020 Jun 7;18(21):3965-3995. doi: 10.1039/d0ob00770f. Epub 2020 May 18.
Cortistatins are a family of steroidal alkaloids with a unique pentacyclic skeleton, having immensely potent anti-angiogenetic activities. Given the scarcity in the natural availability of these compounds, their syntheses became major attractions in organic chemistry. Along with total synthesis of the most potent congeners in the family: cortistatins A and J, the synthesis of two other members have been successfully completed, while various other analogues have also been designed with variable degrees of biological activities. This review is an exhaustive coverage of the significant attempts towards constructing this highly challenging molecule and also aims to highlight the deep understanding of the structure-activity relationships of these compounds, which have been garnered over time.
考地斯塔丁是一类具有独特五环骨架的甾体生物碱，具有极强的抗血管生成活性。鉴于这些化合物在自然界中极为稀缺，它们的合成成为有机化学的主要关注点。除了对家族中最有效同系物考地斯塔丁 A 和 J 的全合成外，还成功完成了另外两个成员的合成，同时还设计了各种具有不同程度生物活性的其他类似物。这篇综述全面介绍了构建这个极具挑战性的分子的重要尝试，并旨在强调随着时间的推移，对这些化合物的结构-活性关系的深入理解。
