Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore
CLF Pooley, JP Edwards, ME Goldman…
Index: Pooley, Charlotte L. F.; Edwards, James P.; Goldman, Mark E.; Wang, Ming-Wei; Marschke, Keith B.; Crombie, Diane L.; Jones, Todd K. Journal of Medicinal Chemistry, 1998 , vol. 41, # 18 p. 3461 - 3466
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Citation Number: 57
Abstract
A series of 6-aryl-1, 2-dihydro-2, 2, 4-trimethylquinolines was synthesized and tested for functional activity on the human progesterone receptor isoform B (hPR-B) in mammalian (CV- 1) cells. The lead compound LG001447 (1, 2-dihydro-2, 2, 4-trimethyl-6-phenylquinoline) was discovered via directed high throughput screening of a defined chemical library utilizing an hPR-B cotransfection assay. Electron-withdrawing substituents at the meta position of ...
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