Discovery of structurally diverse nonsteroidal SPRMs based on a screening hit, 1,2-dihydro-2,2,4-trimethyl-6-phenylquinolinone.
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 side-effects 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.
Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, CA 92121, USA. lzhi@ligand.com
Lin
L
Zhi
D006801:Humans; D011374:Progesterone / Q000031:analogs & derivatives; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D011980:Receptors, Progesterone / Q000187:drug effects*; D013329:Structure-Activity Relationship
C530226:1,2-dihydro-2,2,4-trimethyl-6-phenylquinolinone; D015363:Quinolones; D011980:Receptors, Progesterone; D011374:Progesterone