Potential antineoplastics. 4th communication: N-mustard derivatives of estrone).
The nitrogen mustards 5 and 9 are synthesized as potential mammatropic antineoplastic agents from estrone via 2--4 or 6--8, respectively. 5 and 9 show a binding affinity to the cytoplasmic estrogen receptor of the rat uterus of 1--10% compared to that of estrone. Both mustard compounds are irreversibly bound to the estrogen receptor.
D000818:Animals; D004970:Estrone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism; D005260:Female; D066298:In Vitro Techniques; D009588:Nitrogen Mustard Compounds / Q000138:chemical synthesis* / Q000378:metabolism; D051381:Rats; D011960:Receptors, Estrogen / Q000378:metabolism; D014599:Uterus / Q000378:metabolism
D009588:Nitrogen Mustard Compounds; D011960:Receptors, Estrogen; D004970:Estrone