2. Academic Validation
  3. Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators

Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators

  • Bioorg Med Chem Lett. 2003 Jun 16;13(12):2071-4. doi: 10.1016/s0960-894x(03)00255-5.
Lin Zhi 1,  Christopher M Tegley,  Barbara Pio,  James P Edwards,  Todd K Jones,  Keith B Marschke,  Dale E Mais,  Boris Risek,  William T Schrader
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. lzhi@ligand.com
PMID: 12781197 DOI: 10.1016/s0960-894x(03)00255-5
Abstract

A series of 5-methylidene 1,2-dihydrochromeno[3,4-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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