[芳香酶的新型抑制剂：吡啶基取代菲醌衍生物的合成与生物活性]
[New inhibitors of aromatase: synthesis and biological activity of pyridyl-substituted phenanthrenone derivatives].
作者信息
Bayer H, Hartmann R W
机构信息
Fachrichtung Pharmazeutische Chemie, Universität des Saarlandes.
出版信息
Arch Pharm (Weinheim). 1991 Nov;324(11):833-6. doi: 10.1002/ardp.2503241102.
PMID:1804058
Abstract
The phenanthrenone derivatives 3-6 were synthesized and tested for their aromatase and desmolase inhibitory potency. Compounds 5 and 6 show a stronger inhibition of aromatase than aminoglutethimide not exceeding, however, the activity of the parent compounds 1 and 2. Compounds 4 and 5 do not inhibit desmolase.
摘要
合成了菲醌衍生物3 - 6，并测试了它们对芳香化酶和碳链裂解酶的抑制效力。化合物5和6对芳香化酶的抑制作用比氨鲁米特更强，但未超过母体化合物1和2的活性。化合物4和5不抑制碳链裂解酶。
相似文献
1
[New inhibitors of aromatase: synthesis and biological activity of pyridyl-substituted phenanthrenone derivatives].[芳香酶的新型抑制剂：吡啶基取代菲醌衍生物的合成与生物活性]
Arch Pharm (Weinheim). 1991 Nov;324(11):833-6. doi: 10.1002/ardp.2503241102.
2
[Pyridyl-substituted tetralone derivatives: a new class of nonsteroidal aromatase inhibitors].[吡啶基取代的四氢萘酮衍生物：一类新型非甾体芳香酶抑制剂]
Arch Pharm (Weinheim). 1991 Oct;324(10):815-20.
3
1-Alkyl analogues of aminoglutethimide. Comparative inhibition of cholesterol side chain cleavage and aromatase and metabolism of the 1-propyl derivative, a highly selective inhibitor of aromatase.氨鲁米特的1-烷基类似物。胆固醇侧链裂解和芳香化酶的比较抑制作用以及1-丙基衍生物（一种高度选择性的芳香化酶抑制剂）的代谢。
Biochem Pharmacol. 1988 Jun 1;37(11):2167-72. doi: 10.1016/0006-2952(88)90577-1.
4
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.新型芳香酶抑制剂。吡啶基取代的四氢萘酮衍生物的合成与生物活性
J Med Chem. 1991 Sep;34(9):2685-91. doi: 10.1021/jm00113a004.
5
Analogues of aminoglutethimide: selective inhibition of aromatase.氨鲁米特类似物：芳香化酶的选择性抑制作用
J Med Chem. 1985 Feb;28(2):200-4. doi: 10.1021/jm00380a009.
6
Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.3-环烷基取代的3-(4-氨基苯基)哌啶-2,6-二酮的合成及芳香酶抑制作用
J Med Chem. 1992 Jun 12;35(12):2210-4. doi: 10.1021/jm00090a010.
7
Pharmacology of aminoglutethimide: structure/activity relationships and receptor interactions.
Breast Cancer Res Treat. 1986;7 Suppl:S55-67.
8
Selective inhibition of cholesterol side-chain cleavage by potential pro-drug forms of aminoglutethimide.氨鲁米特潜在前药形式对胆固醇侧链裂解的选择性抑制作用。
Anticancer Drug Des. 1988 Dec;3(3):185-90.
9
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.3-乙基-3-(4-吡啶基)哌啶-2,6-二酮类似物作为芳香酶的选择性抑制剂：具有可变1-烷基和3-烷基取代基的衍生物
J Med Chem. 1987 Sep;30(9):1550-4. doi: 10.1021/jm00392a004.
10
Synthesis and aromatase-inhibitory activity of imidazolyl-1,3,5-triazine derivatives.
Chem Pharm Bull (Tokyo). 1997 Feb;45(2):291-6. doi: 10.1248/cpb.45.291.
Zotero 插件