Bioorganic and Medicinal Chemistry Letters p. 2075 - 2078 (2003)
Update date:2022-08-05
Topics: Pharmacophore Analogues Structure-Activity Relationship (SAR) Studies Clinical Trials Virtual Screening Regulatory Approval Iterative Process In Vitro and In Vivo Testing Functional Group Modifications Pharmacokinetic Optimization Toxicology and Safety Assessment Pharmacophore Identification
Zhi, Lin
Ringgenberg, Josef D.
Edwards, James P.
Tegley, Christopher M.
West, Sarah J.
Pio, Barbara
Motamedi, Mehrnouch
Jones, Todd K.
Marschke, Keith B.
Mais, Dale E.
Schrader, William T.
A series of 1,2-dihydrochromeno[3,4-f]quinoline derivatives was synthesized and tested in biological assays to evaluate the nonsteroidal progesterone receptor modulator pharmacophore (4) as antiprogestins. A number of potent analogues were identified by modification of the substituents at the D-ring.
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