Antiestrogen pharmacology and mechanism of action

The effects of estrogens and antiestrogens on hormone-responsive human breast cancer in long-term tissue culture.

1976 • 820 citations

A MONOHYDROXYLATED METABOLITE OF TAMOXIFEN WITH POTENT ANTIOESTROGENIC ACTIVITY

1977 • 502 citations

Tamoxifen and metabolites in MCF7 cells: correlation between binding to estrogen receptor and inhibition of cell growth.

1982 • 393 citations

High-affinity anti-oestrogen binding site distinct from the oestrogen receptor

1980 • 360 citations

Hydroxylated metabolites of tamoxifen are formed in vivo and bound to estrogen receptor in target tissues.

1981 • 235 citations

Effects of estrogens and antiestrogens on estrogen receptor dynamics and the induction of progesterone receptor in MCF-7 human breast cancer cells.

1982 • 212 citations

Estrogen and Antiestrogen Action in Reproductive Tissues and Tumors

1979 • 194 citations

The Metabolism of Tamoxifen (I.C.I. 46,474) Part I : In Laboratory Animals

1973 • 181 citations

Tamoxifen antiestrogens. A comparison of the activity, pharmacokinetics, and metabolic activation of the cis and trans isomers of tamoxifen

1982 • 169 citations

In Vitro Conversion of Estradiol-Receptor Protein to Its Nuclear Form: Dependence on Hormone and DNA

1972 • 145 citations

Uterine bioassay of tamoxifen, trioxifene and a new estrogen antagonist (LY117018) in rats and mice

1980 • 137 citations

The Metabolism of Tamoxifen (I.C.I. 46,474) Part II: In Female Patients

1973 • 136 citations

Physical properties of estrogen receptor complexes in MCF-7 human breast cancer cells. Differences with anti-estrogen and estrogen.

1982 • 125 citations

Antiestrogen basicity-activity relationships: a comparison of the estrogen receptor binding and antiuterotrophic potencies of several analogs of (Z)-1,2-diphenyl-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-butene (Tamoxifen, Nolvadex) having altered basicity

1982 • 123 citations

High-affinity binding to the estrogen receptor of [3H]4-hydroxytamoxifen, an active antiestrogen metabolite

1980 • 117 citations

Characterization of the 4 S and 5 S Forms of the Estradiol Receptor Protein and Their Interaction with Deoxyribonucleic Acid

1974 • 103 citations

Anti-estrogen interaction with uterine estrogen receptors. Studies with a radiolabeled anti-estrogen (CI-628).

1978 • 103 citations

Synthesis of the (E) and (Z) isomers of the antiestrogen tamoxifen and its metabolite, hydroxytamoxifen, in tritium-labeled form

1982 • 89 citations

The metabolism of tamoxifen in humans

1979 • 87 citations

Antiestrogen specific, high affinity saturable binding sites in rat uterine cytosol

1980 • 72 citations

Interaction of a high affinity anti-estrogen (alpha-[4-pyrrolidinoethoxy]phenyl-4-hydroxy-alpha'-nitrostilbene, CI628M) with uterine estrogen receptors.

1981 • 71 citations

Studies on the metabolism and pharmacokinetics of tamoxifen in normal volunteers.

1980 • 71 citations

Immunopharmacological considerations in Reye's syndrome: A possible xenobiotic initiated disorder?

1978 • 62 citations

The binding of tamoxifen to human mammary carcinoma cytosol

1980 • 59 citations

Antiestrogens: Mechanism of Action and Effects in Breast Cancer

1978 • 55 citations

Biological Potency and Uterine Estrogen Receptor Interactions of the Metabolites of the Antiestrogens CI628 and U23,469*

1981 • 44 citations

Heterogeneity of binding sites for tamoxifen and tamoxifen derivatives in estrogen target and nontarget fetal organs of guinea pig.

1982 • 43 citations

Differential interaction of antiestrogens with cytosol estrogen receptors

1981 • 42 citations

Binding of [³H]Monohydroxytamoxifen by Immature Rat Tissues in Vivo*

1982 • 37 citations

Antiestrogens and antiestrogen metabolites: preparation of tritium-labeled (.+-.)-cis-3-[p-(1,2,3,4-tetrahydro-6-methoxy-2-phenyl-1-naphthyl)phenoxy]-1,2-propanediol and characterization and synthesis of a biologically important metabolite

1979 • 34 citations

Hormones and Their Receptors in Breast Cancer

1978 • 25 citations

Modifications in the aminoether side chain of clomiphene influence affinity for a specific antiestrogen binding site in MCF 7 cell cytosol

1981 • 23 citations

Antitumor activities and estrogen receptor interactions of the metabolites of the antiestrogens C1628 and U23,469 in the 7,12-dimethylbenz(a)anthracene-induced rat mammary tumor system.

1981 • 12 citations

Preparation of tritium‐labeled 4‐hydroxy‐α‐[p‐(2‐(N‐pyrrolidinyl) ethoxy) phenyl]‐α′‐nitrostilbene (CN‐928), a biologically‐important metabolite of the antiestrogen CI‐628

1981 • 11 citations