Jin Chunyang, Manikumar G, Kepler John A, Cook C Edgar, Allan George F, Kiddoe Margaret, Bhattacharjee Sheela, Linton Olivia, Lundeen Scott G, Sui Zhihua
Center for Organic and Medicinal Chemistry, RTI International, PO Box 12194, Research Triangle Park, NC 27709, USA.
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5754-7. doi: 10.1016/j.bmcl.2007.08.064. Epub 2007 Aug 29.
A series of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs have been evaluated for their antagonist hormonal properties using the T47D cell-based alkaline phosphatase assay and the A549 cell-based functional assay. Some of the compounds showed highly potent, and more selective antiprogestational activity against antiglucocorticoid activity than mifepristone (RU 486).
使用基于T47D细胞的碱性磷酸酶测定法和基于A549细胞的功能测定法，对一系列新型11β-芳基-4',5'-二氢螺[雌甾-4,9-二烯-17β,4'-恶唑]类似物的拮抗激素特性进行了评估。一些化合物表现出高效力，并且与米非司酮（RU 486）相比，对糖皮质激素活性具有更高的选择性抗孕激素活性。
