Synthesis and antiandrogenic activity of some new 3-substituted androstano[17,16-c]-5′-aryl-pyrazoline and their derivatives

被引：96

作者：

Amr, AEE ^{[1
]}

Abdel-Latif, NA

Abdalla, MM

机构：

[1] Natl Res Ctr, Appl Organ Chem Dept, Cairo, Egypt

[2] Natl Res Ctr, Nat Cpds Chem Dept, Cairo, Egypt

[3] Egyptian Pharmacist Co, Res Unit, Cairo, Egypt

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 02期

关键词：

pyrazolines; Moffat oxidation; antiandrogenic activity; cyperoterone;

D O I：

10.1016/j.bmc.2005.08.024

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：

A series of androstano[17,16-c]pyrazolines and their oxidized derivatives (2-14) were synthesized using 3 beta-hydroxyandrostan-17-one as a starting material (1a, b). The synthesized compounds were evaluated for their antiandrogenic activity compared to that of Cyproterone (R) as positive control. Some of the compounds exhibited better antiandrogenic activity than the reference drug. The detailed synthesis, spectroscopic data, ED50, and toxicity (LD50 and LD90) of the synthesized compounds were reported. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：373 / 384

页数：12

共 31 条

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