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Microwave-Assisted Hirao and Kabachnik–Fields Phosphorus–Carbon Bond Forming Reactions
Published in Banik Bimal Krishna, Bandyopadhyay Debasish, Advances in Microwave Chemistry, 2018
All the synthesized compounds 6 were evaluated for both their progesterone receptor (PR) antagonist (T47D cell-based assay) and glucocorticoid receptor (GR) antagonist activity (A549 cell-based assay), and their corresponding activities were compared with those of mifepristone, the first competitive progesterone antagonist drug. A selective progesterone receptor (PR) antagonist has potential utility as a contraceptive and also in treating reproductive disorders, such as uterine leiomyomas and endometriosis, and hormone-dependent tumors (Jiang et al., 2006). Hence, the search for some novel class of selective progesterone receptor modulators (PRMs) having only the anti-progestational activity remains highly desirable, both in terms of clinical applications and basic endocrine research. Most of the compounds were potent PR antagonists (nanomolar range), with some showing better selectivity than mifepristone (IC50’s: 0.2 nM (T47D), 2.6 nM (A549); selectivity ratio: 13). Among the series, the most potent molecules were found to be 6a ((IC50’s: 9.9 nM (T47D), 237.7 nM (A549); selectivity ratio: 24), 6b (IC50’s: 3.58 nM (T47D), 660.15 nM (A549); selectivity ratio: 184), and 6c (IC50’s: 1.6 nM (T47D), 270.86 nM (A549); selectivity ratio: 169). In addition, some selected compounds showed modest oral progestin antagonist activity in rat uterus. From the view-point of structure-activity relationship, it was evident that when R1 and R2 are both alkoxy groups, the change in their size did not affect potencies, while a change in the electronics reduced the potency with a more electron-withdrawing group. It was also observed that substitution at the phenyl ring did not significantly change the potency (Jiang et al., 2006).
The right to choose to abort an abortion: should pro-choice advocates support abortion pill reversal?
Published in The New Bioethics, 2022
Michal Pruski, Dominic Whitehouse, Steven Bow
The medical abortion process involves giving an initial dose of mifepristone followed by misoprostol 24-48 h later. Mifepristone is a competitive inhibitor of progesterone, facilitates the dilatation of the cervix, and sensitises the muscles of the uterine wall to the contraction-inducing action of prostaglandin, with the use of this agent alone resulting in the expulsion of the conceptus in circa 60% of cases (Electronic Medicines Compendium 2021a). Misoprostol is a prostaglandin E1 analogue that induces contractions and relaxes the cervix to facilitate the embryo’s expulsion from the womb, which mifepristone alone might not achieve (Electronic Medicines Compendium 2021b).