Wiechert R, Neef G
Research Laboratories, Schering AG, Berlin, F.R.G.
J Steroid Biochem. 1987;27(4-6):851-8. doi: 10.1016/0022-4731(87)90159-2.
The discovery of the first competitive progesterone antagonist RU 38,486 has initiated an intense search for more potent and more selective anti-progestins. Among several hundreds of compounds under preliminary investigation, biological characterization is most advanced for derivatives RU 38,486, ZK 98,734 and ZK 98,299. These compounds do not only differ in relative potency, but are clearly distinguished by their different behaviour in various animal models. Emphasis is laid on the synthetic problems associated with chemical operations in a sterically crowded environment as represented by structures RU 38,486 and ZK 98,299.
首个竞争性孕激素拮抗剂RU 38,486的发现引发了对更强效、更具选择性的抗孕激素的深入探索。在数百种处于初步研究阶段的化合物中，RU 38,486、ZK 98,734和ZK 98,299衍生物的生物学特性研究最为深入。这些化合物不仅在相对效力上有所不同，而且在各种动物模型中的表现也明显不同。重点在于与RU 38,486和ZK 98,299结构所代表的空间拥挤环境中的化学操作相关的合成问题。
