title: Target-directed enediynes: designed estramycins.
abstract: The goal of selective targeting of enediyne cytotoxins has been investigated using estrogenic delivery vehicles. A series of estrogen-enediyne conjugates were assembled, and affinity for human estrogen receptor [hERalpha] was determined. The most promising candidate induced receptor degradation following Bergman cycloaromatization and caused inhibition of estrogen-induced transcription in T47-D human breast cancer cells.
authors.affiliation: Department of Chemistry, Northeastern University, Boston, Massachusetts 02115, USA. grjones@lynx.neu.edu
authors.forename: G B
authors.initials: GB
authors.lastname: Jones
authors.forename: G
authors.initials: G
authors.lastname: Hynd
authors.forename: J M
authors.initials: JM
authors.lastname: Wright
authors.forename: A
authors.initials: A
authors.lastname: Purohit
authors.forename: G W
authors.initials: GW
authors.lastname: Plourde
authors.forename: R S
authors.initials: RS
authors.lastname: Huber
authors.forename: J E
authors.initials: JE
authors.lastname: Mathews
authors.forename: A
authors.initials: A
authors.lastname: Li
authors.forename: M W
authors.initials: MW
authors.lastname: Kilgore
authors.forename: G J
authors.initials: GJ
authors.lastname: Bubley
authors.forename: M
authors.initials: M
authors.lastname: Yancisin
authors.forename: M A
authors.initials: MA
authors.lastname: Brown
mesh_terms: D000480:Alkynes / Q000138:chemical synthesis* / Q000494:pharmacology; D018931:Antineoplastic Agents, Hormonal / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy; D002455:Cell Division / Q000187:drug effects; D003500:Cyclization; D016503:Drug Delivery Systems; D045166:Estradiol Congeners / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D005260:Female; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D011944:Receptors, Androgen / Q000187:drug effects / Q000378:metabolism; D011960:Receptors, Estrogen / Q000187:drug effects / Q000378:metabolism; D014407:Tumor Cells, Cultured
chemical_list: D000480:Alkynes; D018931:Antineoplastic Agents, Hormonal; D045166:Estradiol Congeners; D011944:Receptors, Androgen; D011960:Receptors, Estrogen