Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators |
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| Authors: | Zhi Lin Tegley Christopher M Pio Barbara Edwards James P Jones Todd K Marschke Keith B Mais Dale E Risek Boris Schrader William T |
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| Institution: | Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. lzhi@ligand.com |
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| Abstract: | A series of 5-methylidene 1,2-dihydrochromeno3,4-f]quinoline derivatives were synthesized and tested in biological assays to evaluate scope and limitations of the nonsteroidal SPRM pharmacophore (3). A number of orally available highly potent nonsteroidal modulators were identified by modification of the substituents at 5-methylidene position. |
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