Abstract

Synthetic steroidal progestins and antiprogestins have been widely used for decades to treat many gynecological conditions. The concept of selective progesterone receptor modulators (SPRMs) has been developed in recent years to design new therapeutic agents that have desirable PR modulating activity with significantly reduced sideeffects or increased safety margin. This review describes medicinal chemistry progress of multiple nonsteroidal SPRM series based on a screening hit, 1,2-dihydro-2,2,4-trimethyl-6-phenylquinolinone.

Keywords: Progesterone receptor, mifepristone, antiprogestins, nonsteroidal hPR antagonist, structure activity relationship