11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.
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Rewinkel J, Enthoven M, Golstein I, van der Rijst M, Scholten A, van Tilborg M, de Weys D, Wisse J, Hamersma H
11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.
Bioorg Med Chem. 2008 Mar 15;16(6):2753-63. doi: 10.1016/j.bmc.2008.01.010. Epub 2008 Jan 11.
- PubMed ID
- 18243712 [ View in PubMed]
- Abstract
Recently, a new class (often referred to as SPRMs: selective progesterone receptor modulators) of progesterone receptor ligands with mixed agonist/antagonist properties has been described. Such compounds are envisaged, for example, as treatment for endometriosis, uterine fibroids, and leiomyomas. Existing SPRMs include Asoprisnil 1 and Uliprisnil acetate 2. In our hands, however, these compounds proved to have a predominantly or exclusively antagonistic in vitro profile, which may make this type of compound less attractive, for example, as contraceptives. We therefore aimed at a class of mixed-profile compounds that would show a more evenly balanced agonist/antagonist profile. A novel class of 11beta-[4-(heteroaryl)phenyl]-substituted pregnanes was identified that displayed the desired balance. Contrary to known SPRMs, this novel class of MPP (mixed-profile progestagen) was found to have a truly mixed activity, including a sizeable agonist component.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Ulipristal Progesterone receptor EC 50 (nM) >100 N/A N/A Details Ulipristal Progesterone receptor IC 50 (nM) 0.2 N/A N/A Details