作者: Ken-ichi Kurihara , Kiyoshi Tanabe , Yasuo Yamamoto , Rie Shinei , Keiichi Ajito
DOI: 10.1016/S0960-894X(99)00275-9
关键词: Methyl group 、 Chemistry 、 Progesterone receptor 、 Non steroidal 、 Stereochemistry 、 Lactone 、 Chemical synthesis 、 In vitro
摘要: Abstract In order to study structure-activity relationships, a series of new non-steroidal progesterone receptor ligands based on PF1092A 1) was synthesized with structural modifications (mostly introduction or removal methyl group) at the 3-, 4-, 5-, 7- 9-position in 6-acetoxy-4a, 5, 6, 7-tetrahydro-3, 4a, 5-trimethylnaphtho[2, 3 - b ]furan-2(4 H )-one 2) skeleton. Critical positions for high binding affinity were identified.