2-phenylspiroindenes: A novel class of Selective Estrogen Receptor Modulators (SERMs)

被引:36
作者
Blizzard, TA [1 ]
Morgan, JD [1 ]
Mosley, RT [1 ]
Birzin, ET [1 ]
Frisch, K [1 ]
Rohrer, SP [1 ]
Hammond, ML [1 ]
机构
[1] Merck Res Labs, Rahway, NJ 07065 USA
关键词
D O I
10.1016/S0960-894X(02)00985-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 2-phenylspiroindenes was prepared. The most active analogue (2) was found to be comparable in potency to raloxifene (1) as an estrogen receptor ligand. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:479 / 483
页数:5
相关论文
共 26 条
[1]   Molecular basis of agonism and antagonism in the oestrogen receptor [J].
Brzozowski, AM ;
Pike, ACW ;
Dauter, Z ;
Hubbard, RE ;
Bonn, T ;
Engstrom, O ;
Ohman, L ;
Greene, GL ;
Gustafsson, JA ;
Carlquist, M .
NATURE, 1997, 389 (6652) :753-758
[2]   Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women [J].
Delmas, PD ;
Bjarnason, NH ;
Mitlak, BH ;
Ravoux, AC ;
Shah, AS ;
Huster, WJ ;
Draper, M ;
Christiansen, C .
NEW ENGLAND JOURNAL OF MEDICINE, 1997, 337 (23) :1641-1647
[3]   ACCESS TO THE SPIRO HYDRINDANDIONE RING-SYSTEM OF FREDERICAMYCIN-A THROUGH SPIROALKYLATION AND OXIDATION [J].
ECK, G ;
JULIA, M ;
PFEIFFER, B ;
ROLANDO, C .
TETRAHEDRON LETTERS, 1985, 26 (39) :4725-4726
[4]   1-ARYL-3-AZABICYCLO[3.1.0]HEXANES, A NEW SERIES OF NON-NARCOTIC ANALGESIC AGENTS [J].
EPSTEIN, JW ;
BRABANDER, HJ ;
FANSHAWE, WJ ;
HOFMANN, CM ;
MCKENZIE, TC ;
SAFIR, SR ;
OSTERBERG, AC ;
COSULICH, DB ;
LOVELL, FM .
JOURNAL OF MEDICINAL CHEMISTRY, 1981, 24 (05) :481-490
[5]   Molecular determinants of tissue selectivity in estrogen receptor modulators [J].
Grese, TA ;
Sluka, JP ;
Bryant, HU ;
Cullinan, GJ ;
Glasebrook, AL ;
Jones, CD ;
Matsumoto, K ;
Palkowitz, AD ;
Sato, M ;
Termine, JD ;
Winter, MA ;
Yang, NN ;
Dodge, JA .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1997, 94 (25) :14105-14110
[6]   Synthesis and pharmacology of conformationally restricted raloxifene analogues: Highly potent selective estrogen receptor modulators [J].
Grese, TA ;
Pennington, LD ;
Sluka, JP ;
Adrian, MD ;
Cole, HW ;
Fuson, TR ;
Magee, DE ;
Phillips, DL ;
Rowley, ER ;
Shetler, PK ;
Short, LL ;
Venugopalan, M ;
Yang, NN ;
Sato, M ;
Glasebrook, AL ;
Bryant, HU .
JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (08) :1272-1283
[7]   Synthesis and isolation of some benzo[c]tellurophenes [J].
Huang, ZZ ;
Lakshmikantham, MV ;
Lyon, M ;
Cava, MP .
JOURNAL OF ORGANIC CHEMISTRY, 2000, 65 (17) :5413-5415
[8]   ANTIESTROGENS .2. STRUCTURE ACTIVITY STUDIES IN A SERIES OF 3-AROYL-2-ARYLBENZO[B]THIOPHENE DERIVATIVES LEADING TO [6-HYDROXY-2-(4-HYDROXYPHENYL)BENZO[B]THIEN-3-YL][4-[2-(1-PIPERIDINYL)ETHOXY]-PHENYL]METHANONE HYDROCHLORIDE (LY156758), A REMARKABLY EFFECTIVE ESTROGEN ANTAGONIST WITH ONLY MINIMAL INTRINSIC ESTROGENICITYO[ [J].
JONES, CD ;
JEVNIKAR, MG ;
PIKE, AJ ;
PETERS, MK ;
BLACK, LJ ;
THOMPSON, AR ;
FALCONE, JF ;
CLEMENS, JA .
JOURNAL OF MEDICINAL CHEMISTRY, 1984, 27 (08) :1057-1066
[9]  
JORDAN C, 1998, SCI AM OCT, P60