Synthesis and evaluation of 17-alpha-heteroarylvinyl estradiols as ligands for the estrogen receptor ligand binding domain (ER-LBD)

被引:0
|
作者
Olmsted, Sandra [1 ]
Hanson, Robert N. [2 ]
Tongcharoensirikul, Pakamas [2 ]
McCaskill, Emmett [2 ]
Hochberg, Richard B. [3 ]
Labaree, David C. [3 ]
机构
[1] Augsburg Coll, Dept Chem, Minneapolis, MN 55454 USA
[2] Northeastern Univ, Dept Chem & Chem Biol, Boston, MA 02115 USA
[3] Yale Univ, Sch Med, Dept Obstet & Gynecol, New Haven, CT 06510 USA
关键词
D O I
暂无
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
373-MEDI
引用
收藏
页码:711 / 711
页数:1
相关论文
共 50 条
  • [31] Molecular dynamics studies of (17alpha,20E)-21-(2-/3-/4substituted phenyl)-19-norpregna-1,3,5(10),20-tetraene-3,17betadiols as ligands for the estrogen receptor-alpha-ligand binding domain (ERalpha-LBD).
    Hanson, RN
    Dilis, R
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 229 : U137 - U137
  • [32] SYNTHESIS AND EVALUATION OF 17-ALPHA-[I-125]IODOVINYLESTRADIOL - A POTENTIAL ESTROGEN-RECEPTOR RADIOLIGAND
    HANSON, RN
    SEITZ, DE
    TRANSACTIONS OF THE AMERICAN NUCLEAR SOCIETY, 1981, 39 : 32 - 33
  • [33] Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-α)
    Singla, Ramit
    Gupta, Kunj Bihari
    Upadhyay, Shishir
    Dhiman, Monisha
    Jaitak, Vikas
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 146 : 206 - 219
  • [34] Change in selectivity of estrogen receptor alpha ligand-binding domain by mutations at residues H524/L525
    Arevalo-Salina, Emma L.
    Nishigaki, Takuya
    Olvera, Leticia
    Gonzalez-Andrade, Martin
    Xolalpa-Villanueva, Wendy
    Lopez-Romero, Edith O.
    Soberon, Xavier
    Saab-Rincon, Gloria
    BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS, 2025, 1869 (04):
  • [35] In Silico Identification and Pharmacological Evaluation of Novel Endocrine Disrupting Chemicals That Act via the Ligand-Binding Domain of the Estrogen Receptor α
    McRobb, Fiona M.
    Kufareva, Irina
    Abagyan, Ruben
    TOXICOLOGICAL SCIENCES, 2014, 141 (01) : 188 - 197
  • [36] Estrogen receptor alpha (ERα)-mediated coregulator binding and gene expression discriminates the toxic ERα agonist diethylstilbestrol (DES) from the endogenous ERα agonist 17β-estradiol (E2)
    Adam, Aziza Hussein Bakheit
    de Haan, Laura H. J.
    Estruch, Ignacio Miko
    Hooiveld, Guido J. E. J.
    Louisse, Jochem
    Rietjens, Ivonne M. C. M.
    CELL BIOLOGY AND TOXICOLOGY, 2020, 36 (05) : 417 - 435
  • [37] Estrogen receptor alpha (ERα)–mediated coregulator binding and gene expression discriminates the toxic ERα agonist diethylstilbestrol (DES) from the endogenous ERα agonist 17β-estradiol (E2)
    Aziza Hussein Bakheit Adam
    Laura H. J. de Haan
    Ignacio Miro Estruch
    Guido J. E. J. Hooiveld
    Jochem Louisse
    Ivonne M. C. M. Rietjens
    Cell Biology and Toxicology, 2020, 36 : 417 - 435
  • [38] POINT MUTATION OF ESTROGEN-RECEPTOR (ER) IN THE LIGAND-BINDING DOMAIN CHANGES THE PHARMACOLOGY OF ANTIESTROGENS IN ER-NEGATIVE BREAST-CANCER CELLS STABLY EXPRESSING COMPLEMENTARY DNAS FOR ER
    JIANG, SY
    LANGANFAHEY, SM
    STELLA, AL
    MCCAGUE, R
    JORDAN, VC
    MOLECULAR ENDOCRINOLOGY, 1992, 6 (12) : 2167 - 2174
  • [39] X-ray crystal structure analysis of elacestrant (RAD1901), a novel selective estrogen receptor degrader (SERD), bound to estrogen receptor alpha ligand binding domain.
    Fanning, Sean W.
    Greene, Geoffrey
    Conlan, Maureen G.
    JOURNAL OF CLINICAL ONCOLOGY, 2020, 38 (15)
  • [40] Investigation of a Radio-Iodinated Alpha-Mangostin for Targeting Estrogen Receptor Alpha (ERα) in Breast Cancer: In Silico Design, Synthesis, and Biological Evaluation
    Muchtaridi, Muchtaridi
    Nurhidayah, Wiwit
    Fakih, Taufik Muhammad
    Kannaka, Kento
    Suzuki, Hiroyuki
    Subroto, Toto
    Uehara, Tomoya
    DRUG DESIGN DEVELOPMENT AND THERAPY, 2024, 18 : 4511 - 4526