Synthesis and estrogen receptor binding affinities of novel pyrrolo[2,1,5-cd]indolizine derivatives

被引：48
作者：
Jorgensen, AS [1 ]
Jacobsen, P [1 ]
Christiansen, LB [1 ]
Bury, PS [1 ]
Kanstrup, A [1 ]
Thorpe, SM [1 ]
Nærum, L [1 ]
Wassermann, K [1 ]
机构：
[1] Novo Nordisk AS, Hlth Care Discovery & Preclin Dev, DK-2760 Malov, Denmark
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 20期
关键词：
D O I：
10.1016/S0960-894X(00)00474-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of pyrrolo[2,1,5-cd]indolizine derivatives has been synthesized and evaluated as ligands for the estrogen receptor. Properly substituted mono- and di-hydroxy derivatives showed binding in the low nanomolar range in accordance with their structural resemblance to estrogen. (C) 2000 Elsevier Science Ltd. All rights reserved.
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收藏
页码：2383 / 2386
页数：4
相关论文
共 23 条
  • [1] The estradiol pharmacophore: Ligand structure-estrogen receptor binding affinity relationships and a model for the receptor binding site
    Anstead, GM
    Carlson, KE
    Katzenellenbogen, JA
    [J]. STEROIDS, 1997, 62 (03) : 268 - 303
  • [2] Effect of testosterone and estradiol in a man with aromatase deficiency
    Carani, C
    Qin, K
    Simoni, M
    FaustiniFustini, M
    Serpente, S
    Boyd, J
    Korach, KS
    Simpson, ER
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 1997, 337 (02) : 91 - 95
  • [3] THE USE OF ESTROGENS AND PROGESTINS AND THE RISK OF BREAST-CANCER IN POSTMENOPAUSAL WOMEN
    COLDITZ, GA
    HANKINSON, SE
    HUNTER, DJ
    WILLETT, WC
    MANSON, JE
    STAMPFER, MJ
    HENNEKENS, C
    ROSNER, B
    SPEIZER, FE
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 1995, 332 (24) : 1589 - 1593
  • [4] Cosman Felicia, 1997, P151
  • [5] Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women
    Delmas, PD
    Bjarnason, NH
    Mitlak, BH
    Ravoux, AC
    Shah, AS
    Huster, WJ
    Draper, M
    Christiansen, C
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 1997, 337 (23) : 1641 - 1647
  • [6] ENDO M, 1960, YAKUGAKU ZASSHI, V80, P875
  • [7] The vascular protective effects of estrogen
    Farhat, MY
    Lavigne, MC
    Ramwell, PW
    [J]. FASEB JOURNAL, 1996, 10 (05) : 615 - 624
  • [8] *SYNTHESE DES D-PSEUDOCONHYDRINS
    GRUBER, W
    SCHLOGL, K
    [J]. MONATSHEFTE FUR CHEMIE, 1949, 80 (04): : 499 - 505
  • [9] A genetic algorithm for flexible molecular overlay and pharmacophore elucidation
    Jones, G
    Willett, P
    Glen, RC
    [J]. JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN, 1995, 9 (06) : 532 - 549
  • [10] Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor
    Jorgensen, AS
    Jacobsen, P
    Christiansen, LB
    Bury, PS
    Kanstrup, A
    Thorpe, SM
    Bain, S
    Nærum, L
    Wassermann, K
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (04) : 399 - 402
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