Synthesis and structure-activity relationships of new non-steroidal progesterone receptor ligands

In order to study structure-activity relationships, a series of new non-ste roidal progesterone receptor ligands based on PF1092A (1)) was synthesized with structural modifications (mostly introduction or removal of a methyl g roup) at the 3-, 4-, 5-, 7- or 9-position in the 6-acetoxy-4a, 5, 6, 7-tetr ahydro-3, 4a, 5-trimethylnaphtho[2, 3-b]furan-2(4H)-one (2)) skeleton. Crit ical positions for high binding affinity to the progesterone receptor were identified. (C) 1999 Elsevier Science Ltd. All rights reserved.