Synthesis and relative binding affinity to steroid receptors and antiproliferative activity on MCF-7 cells of 2,3-disubstituted indenes

被引：2
作者：
Kirkiacharian, S
Koutsourakis, PG
Philibert, D
Bouchoux, F
Van de Velde, P
机构：
[1] Fac Pharm Paris Sud, Chim Therapeut Lab, F-92226 Chatenay Malabry, France
[2] Grp HMR, Lab Physiol Hormones, Labs Roussel, F-93230 Romainville, France
来源：
FARMACO | 1999年 / 54卷 / 10期
关键词：
binding affinity; steroid receptor; antiproliferative activity;
D O I：
10.1016/S0014-827X(99)00080-4
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The study of the relative binding affinity of a set of 2,3-disubstituted indenes to the receptors of steroid hormones indicates a weak effect of some derivatives on estrogen, progesterone and androgen receptors. The antiproliferative effect on human MCF-7 cells also shows a weak activity for three derivatives. (C) 1999 Elsevier Science S.A. All rights reserved.
引用
收藏
页码：678 / 683
页数：6
相关论文
共 29 条
[1]  
ACTON D, 1998, DRUGS FUTURE, V23, P792
[2]  
ACTON D, 1983, J MED CHEM, V31, P1131
[3]   TORSIONALLY AND HYDROPHOBICALLY MODIFIED 2,3-DIARYLINDENES AS ESTROGEN-RECEPTOR LIGANDS [J].
ANSTEAD, GM ;
PETERSON, CS ;
PINNEY, KG ;
WILSON, SR ;
KATZENELLENBOGEN, JA .
JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (10) :2726-2734
[4]   CHROMIC ACID OXIDATION OF ORGANOBORANES-CONVENIENT PROCEDURE FOR CONVERTING OLEFINS INTO KETONES VIA HYDROBORATION [J].
BROWN, HC ;
GARG, CP .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1961, 83 (13) :2951-&
[5]  
DUNCAN GW, 1963, P SOC EXP BIOL MED, V112, P439
[6]  
FEVIG D, 1988, J MED CHEM, V31, P1754
[7]  
FRAZER MJ, 1989, CELL DEV BIOL, V25, P225
[8]  
Grese TA, 1998, CURR PHARM DESIGN, V4, P71
[9]   ANTIESTROGENS .3. ESTROGEN-RECEPTOR AFFINITIES AND ANTIPROLIFERATIVE EFFECTS IN MCF-7 CELLS OF PHENOLIC ANALOGS OF TRIOXIFENE, [3,4-DIHYDRO-2-(4-METHOXYPHENYL)-1-NAPHTHALENYL][4-[2-(1-PYRROLIDINYL)ETHOXY]-PHENYL]METHANONE [J].
JONES, CD ;
BLASZCZAK, LC ;
GOETTEL, ME ;
SUAREZ, T ;
CROWELL, TA ;
MABRY, TE ;
RUENITZ, PC ;
SRIVATSAN, V .
JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (05) :931-938
[10]   SYNTHESIS AND ANTI-ESTROGENIC ACTIVITY OF [3,4-DIHYDRO-2-(4-METHOXYPHENYL)-1-NAPHTHALENYL][4-[2-(1-PYRROLIDINYL)ETHOXY]PHENYL]METHANONE, METHANESULFONIC-ACID SALT [J].
JONES, CD ;
SUAREZ, T ;
MASSEY, EH ;
BLACK, LJ ;
TINSLEY, FC .
JOURNAL OF MEDICINAL CHEMISTRY, 1979, 22 (08) :962-966
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