| Autor: |
Tegley, C. M., Zhi, L., Marschke, K. B., Gottardis, M. M., Yang, Q., Jones, T. K. |
| Zdroj: |
Journal of Medicinal Chemistry; October 22, 1998, Vol. 41 Issue: 22 p4354-4359, 6p |
| Abstrakt: |
A novel series of nonsteroidal progestins, 5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines (2), was discovered, and a preliminary structure−activity relationship study around the 5-benzylidene ring generated several potent human progesterone receptor agonists (compounds 8, 16). These new progestins showed biological activities (EC50 = 5.7 and 7.6 nM) similar to progesterone (EC50 = 2.9 nM) in the cotransfection assay with high efficacy (132% and 166%) and binding affinity (Ki = 0.66 and 0.83 nM) similar to medroxyprogesterone acetate (MPA) (Ki = 0.34 nM). A representative analogue, 8, demonstrated similar oral potency to MPA in the uterine wet weight/mammary gland morphology assay in ovariectomized rats. |
| Databáze: |
Supplemental Index |
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