Structure-activity relationships of estrogens.
Structure-activity relationships of 9 beta-estrogens. Except for ethinyl-9 beta -estradiol beta which was as active as its 9a isomer in the uterotropic assay. SAR. Steroidal Estrogenic Drugs. Estradiol: Most active natural estrogen. Very short duration of Ethinyl estradiol (α-ethynylestradiol). 20 more potent. Studies of structure-activity relationships in vivo using Allen Doisy or 3-day uterine . [PubMed]; Eisenfeld A. Oral contraceptives: ethinyl estradiol binds with .
Estra-1,3,5 10 triene-3,diol 8 Nonsteroidal Estrogens 1. The trans form is the active one. As active as Estradiol. Longer duration of action. Increase the risk of uterine cancer. Treatment of prostate cancer. Active orally 10 Xenoestrogens Enviromental Estrogens Estrogenic compounds with weak activity present in food and drinks. Isoflavones and coumestrol Coumestan derivatives present in family Leguminosae are examples of xenoestrogens.
Structure-activity relationships of 9 beta-estrogens.
Treatment of estrogen dependent cancers. They are related to stilbene in structure. Antagonist bind strongly to the receptors. Block conversion of androgens to estrogens. By the ovary mainly the corpus luteum during the second half of the menstrual cycle. Development of the endometrium. Development of the mammary gland during pregnancy.
Milk secretion starts when its level decrease with birth. Have some androgenic activity. Removal of the 19 CH3 increase activity. Unsaturation of ring B or C increase the activity.
Removal of the keto function remove androgenic activity. Semisynthetic progestin with pure progestrogenic activity. Endometrial, renal and breast carcinoma. Enhance respiration for Hypoventilation. Nausea, vomiting, irregular bleeding, edema, weight gain, breakthrough bleeding, breast discomfort. Compete with the progestin receptors.
Sodium and water retention leads to edema. FSH stimulates sperm production LH stimulates secretion of testosterone. Androgens possess anabolic activity. Treament of breast cancer in menopausal women. Cholestatic jaundice Enlargement of prostate Atherosclerosis Hepatic carcinoma Oedema 25 2.
Structure-activity relationships of estrogens.
The use of triphenyltetrazolium chloride in the biological assay of oestrogens. The estimation of oestrin and of male hormone in oily solution. Bioassay of estrogens using the mouse uterine response.
Uptake of radioactive oestradiol in some organs of immature mice. The capacity and structural specificity of uptake studied with several steroid hormones. Acta Endocrinol Copenh Dec;50 4: Effect of synthetic oestrogens and analogues on the uptake of oestradiol by the immature mouse uterus and vagina. Acta Pharmacol Toxicol Copenh ;24 1: Prolonged antioestrogenic activity of ICI 46, in the ovariectomized mouse.
The binding of [3H]-oestradiol beta in the immature rat uterus during the sequential administration of non-steroidal anti-oestrogens.
An estrogen receptor model to describe the regulation of prolactin synthesis by antiestrogens in vitro. Comparative binding affinity of estrogens and its relation to estrogenic potency.
Number of Nuclear Positions and Steroid Classification
Molecular parameters involved in the estrogenicity of mestranol and ethynylestradiol. Evidence for the metabolic activation of non-steroidal antioestrogens: Estrogen control of prolactin synthesis in vitro. Direct and reversible inhibition of estradiol-stimulated prolactin synthesis by antiestrogens in vitro. Primary cultures of estrogen-responsive cells from rat uteri: A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. Modulation of rat uterine steroid hormone receptors by estrogen and antiestrogen.
Subcellular effects of monohydroxytamoxifen in the rat uterus: Potential value of plants as sources of new antifertility agents II. Phytoestrogen interaction with estrogen receptors in human breast cancer cells. Estrogens and related substances in plants. Steroid and phyto-oestrogen binding to sheep uterine receptors in vitro. Estrogenic activity of some isoflavone derivatives.
The effects of plant oestrogens on animal reproduction. Excretion, isolation and structure of a new phenolic constituent of female urine. Lignans in man and in animal species.Morphine Structure Activity Relationship
Origin of lignans in mammals and identification of a precursor from plants. Oestrogen-responsive human breast cancer in long term tissue culture. Estrogenic activity of some flavonoids. Coumestrol, a new estrogen isolated from forage crops. Binding characteristics of zearalenone analogs to estrogen receptors.
Mechanism of Fusarium mycotoxin action in mammary gland. J Toxicol Environ Health. Effects of pesticides and related compounds on steroid metabolism and function. Estrogenic activities of chlorinated hydrocarbons. Estrogenic action of DDT analogs.