Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens

Journal of Medicinal Chemistry

Volumn 44, Issue 11, 2001, Pages 1654-1657

  Miller, C P ^a   Collini, M D ^a   Tran, B D ^a   Harris, H A ^a   Kharode, Y P ^a   Marzolf, J T ^a   Moran, R A ^a   Henderson, R A ^a   Bender, R H W ^a   Unwalla, R J ^a   Greenberger, L M ^a   Yardley, J P ^a   Abou Gharbia, M A ^a   Lyttle, C R ^a   Komm, B S ^a  

^a WYETH AYERST RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BAZEDOXIFENE; DIETHYLSTILBESTROL; ESTRADIOL; ESTROGEN DERIVATIVE; PIPENDOXIFENE; RALOXIFENE; TAMOXIFEN; UNCLASSIFIED DRUG; ZK 119010;

DRUG STRUCTURE; DRUG SYNTHESIS; HORMONE SUBSTITUTION; LETTER; MENOPAUSE; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ANIMALS; BONE DENSITY; CELL LINE; ESTRADIOL CONGENERS; FEMALE; INDOLES; MODELS, MOLECULAR; ORGAN SIZE; OVARIECTOMY; RADIOLIGAND ASSAY; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSFECTION; UTERUS;

EID: 0035942513     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010086m     Document Type: Letter

References (19)

1. Current perspectives on the benefits of HRT in menopausal women
2. Hormone replacement therapy and breast cancer
3. Endometrial cancer. Prevention, detection, management, and follow up
4. Postmenopausal hormone therapy and the risk of breast cancer
5. Selective estrogen receptor modulators (SERMs)
6. Effects of anti-estrogens on bone in castrated and intact female rats
7. Estradiol derivatives bearing the side-chain of tamoxifen antagonize the association between the estrogen receptor and calmodulin
8. Molecular basis of agonism and antagonism in the estrogen receptor
9. The structural basis of oestrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen
10. Molecular determinants of tissue selectivity in estrogen receptor modulators
11. Pharmacological characterization of a novel estrogen antagonist, ZK 119010, in rats and mice
12. 2-Phenylindoles. Relationship between structure, estrogen receptor affinity, and mammary tumor inhibiting activity in the rat
13. Syntheis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives
14. Suppression of ligand-dependent estrogen receptor activity by bone-resorbing cytokines in human osteoblasts
15. Tripartite steroid hormone receptor pharmacology: Interaction with multiple effector sites as a basis for the cell- and promoter-specific action of these hormones
16. Structure-activity relationships of selective estrogen receptor modulators: Modifications to the 2-aryl-benzothiophene core of raloxifene
17. The effect of conjugated equine estrogens on ovariectomy-induced osteopenia in the rat
18. 2-Phenylindoles with sulfur containing side chains. Estrogen receptor affinity, antiestrogenic potency, and antitumor activity
19. Comparison of ERA-923, a new selective estrogen receptor modulator (SERM) for the treatment of estrogen-receptor positive breast cancer, with other SERMs