Novel non-steroidal/non-anilide type androgen antagonists with an isoxazolone moiety

被引：113

作者：

Ishioka, T

Kubo, A

Koiso, Y

Nagasawa, K

Itai, A

Hashimoto, Y

机构：

[1] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 1130032, Japan

[2] Key Mol Inc, Inst Med Mol Design, Bunkyo Ku, Tokyo 1130033, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 05期

关键词：

D O I：

10.1016/S0968-0896(01)00421-7

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

3-Substitutcd (Z)-4-(4-N,N-dialkylaminophenylmethylene)-5(4H)-isoxazolones and related compounds were designed and prepared as candidates for structurally novel androgen antagonists. Several compounds showed potent anti-androgenic activity as assessed by nuclear androgen receptor binding assay and growth inhibition assay using androgen-dependent Shionogi carcinoma cells SC-3. They were approximately 10-220 times more potent than flutamide in these assay systems, They also showed anti-androgenic activity toward prostate tumor cell line LNCaP, which has an aberrant nuclear androgen receptor. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1555 / 1566

页数：12

共 33 条

[1] Mouse fibroblast growth factor 10: cDNA cloning, protein characterization, and regulation of mRNA expression [J].