[Synthetic estrogens--new pharmacological actions and mechanisms].
Many constitutional analogues of estrogen have been reported. In this review, some new synthetic estrogens possessing a different action from natural estrogens are described. Aminoestrogens inhibit platelet aggregation. Estradiol-chlorambucil conjugate (KM2210) decreases the level of estrogen receptor mRNA in the human breast cancer cell MCF-7. The representative synthetic estrogen, diethylstilbestrol, and its derivatives show an inhibitory action against H(+)- and Ca(2+)-ATPase. Moreover, the effect of the diastereometric [1,2-bis(2,6-dihalo-3-hydroxyphenyl)ethylenediamine ] sulfatoplatinum (II) complexes, derivatives of hexesterol-platinum complexes, on estrogenic action and the growth-inhibitory action of hormone dependent breast cancer, are strongly dependent on the halogen atoms and on their position in the aromatic ring. These drugs are expected to be applicable for clinical use.
Kosano
H
H
Faculty of Pharmaceutical Sciences, Teikyo University.
Nishigori
H
H
D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy / Q000378:metabolism; D000252:Calcium-Transporting ATPases / Q000037:antagonists & inhibitors; D015195:Drug Design; D045166:Estradiol Congeners / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D012333:RNA, Messenger / Q000378:metabolism; D011960:Receptors, Estrogen / Q000378:metabolism
D045166:Estradiol Congeners; D010975:Platelet Aggregation Inhibitors; D012333:RNA, Messenger; D011960:Receptors, Estrogen; D000252:Calcium-Transporting ATPases