ChemInform Abstract: SYNTHESIS OF Ω‐BROMO KETONES

House, Herbert O.; Chu, Chia-Yeh; Phillips, William V.; Sayer, Trevor S. B.; Yau, Cheuk-Chung

doi:10.1002/chin.197742129

Cited by 1 publication

(1 citation statement)

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“…16 Conjugate addition of methyl cuprate to enone 7a, followed by Peterson methylenation/desilylation, gave 9. Similarly, conjugate addition of vinyl cuprate 17 to enone 7a allowed installation of varied functionality at this position. Ozonolysis of the vinyl group gave an aldehyde which was selectively reduced using lithium tris[(3ethyl-3-pentyl)oxy]aluminohydride (LiTEPA) 18 to afford the corresponding primary alcohol.…”

Section: Chemistrymentioning

confidence: 99%

Synthesis and Biological Activity of Novel Nonsteroidal Progesterone Receptor Antagonists Based on Cyclocymopol Monomethyl Ether

et al. 1996

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A novel class of nonsteroidal progesterone receptor antagonists has been synthesized and was shown to exhibit moderate binding affinity for hPR-A, the ability to inhibit the transcriptional activity of human progesterone receptor (hPR) in cell-based assays, and anti-progestational activity in a murine model. Cyclocymopol monomethyl ether, a component of the marine alga Cymopolia barbata was weakly active in random screening against PR. Investigations into the SAR surrounding the core of this natural product lead structure resulted in improved in vitro activity. In contrast to the cross-reactivity profiles observed with known steroidal antiprogestins, compounds of the general structural class described display a high degree of selectivity for the progesterone receptor and no functional activity on the glucocorticoid receptor.

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Section: Chemistrymentioning

confidence: 99%