ABSTRACT
AIM In order to improve the biological activity and reduce the side effects and toxicity, a series of novel estrogen receptor antagonists were designed. METHODS The key triphenylethylene intermediates were obtained by the McMurry reaction. The target compounds were prepared by etherification. The binding affinities of the target compounds for the estrogen receptor in rat uterine cytosol were measured by a competitive binding assay and their estrogen agonistic/antagonistic properties were investigated in the 3-day uterine weight assay in the immature rats. RESULTS Thirty-five new compounds have been synthesized and their geometric configuration were determined by X-ray crystallography and 1HNMR spectral data. CONCLUSION All of the test compounds showed affinity for the estrogen receptor (IC50<10-6 mol.L-1), especially compound 35 with IC50 1.07×10-8 mol.L-1. Some compounds are antagonists, inhibiting uterus growth; others are agonists, promoting uterus growth. Compounds 14 and 27 are superior antagonists to tamoxifen.
ABSTRACT
Misoprostol, a prostaglandin E1 analogue, have variety clinical applications. In early 80's, misoprostol is currently licensed primarily to prevent non-steroidal anti-inflammatory drug-associated gastric and duodenal ulcers. Further work shows the drugs have protection to hepatic and renal and prevention of inflammatory and allergic disorders. When combined with mifepristone,complete abortion rate is 95%. On the other hand, misoprostol is also an effective agent for cervical ripening and labor induction. It have no serious side effect, as a result, misoprostol is a drug of high effect and low toxicity, deserving popularization, but man and pregnant woman must prudent.