Suppr超能文献

Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES).

作者信息

Ahmed S, James K, Owen C P, Patel C K, Patel M

机构信息

School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, KT1 2EE, Surrey, UK.

出版信息

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2525-8. doi: 10.1016/s0960-894x(01)00482-6.

DOI:10.1016/s0960-894x(01)00482-6
PMID:11549461
Abstract

We report the initial structure-activity relationship study (SAR) (in particular logP) of a series of compounds based upon 4-sulfamated phenyl ketones as potent inhibitors of the enzyme estrone sulfatase (ES). The results of the study show that these compounds are irreversible inhibitors of ES and that they are more potent than COUMATE, but weaker than EMATE. Analysis of the SAR data shows a strong correlation between IC(50) and logP but also supports our previous study, which suggests a very strong relationship between pK(a) and IC(50).

摘要

相似文献

1
Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES).
Bioorg Med Chem Lett. 2001 Sep 17;11(18):2525-8. doi: 10.1016/s0960-894x(01)00482-6.
2
The design, synthesis, and biochemical evaluation of derivatives of biphenyl sulfamate-based compounds as novel inhibitors of estrone sulfatase.基于联苯氨基磺酸酯的化合物衍生物作为新型雌酮硫酸酯酶抑制剂的设计、合成及生化评价
Biochem Biophys Res Commun. 2002 May 31;294(1):180-3. doi: 10.1016/S0006-291X(02)00444-8.
3
Novel inhibitors of the enzyme estrone sulfatase (ES).
Bioorg Med Chem Lett. 2001 Mar 26;11(6):841-4. doi: 10.1016/s0960-894x(01)00086-5.
4
Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES).
J Steroid Biochem Mol Biol. 2002 Nov;82(4-5):425-35. doi: 10.1016/s0960-0760(02)00228-5.
5
Synthesis and biochemical evaluation of novel and potent inhibitors of the enzyme oestrone sulphatase (ES).
J Steroid Biochem Mol Biol. 2002 Apr;80(4-5):419-27. doi: 10.1016/s0960-0760(02)00037-7.
6
Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism.
Bioorg Med Chem Lett. 2001 Dec 3;11(23):3001-5. doi: 10.1016/s0960-894x(01)00607-2.
7
Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES).
Bioorg Med Chem Lett. 2002 May 20;12(10):1343-6. doi: 10.1016/s0960-894x(02)00170-1.
8
Steroidal and nonsteroidal sulfamates as potent inhibitors of steroid sulfatase.甾体和非甾体氨基磺酸酯作为类固醇硫酸酯酶的有效抑制剂。
J Med Chem. 1998 Mar 26;41(7):1068-83. doi: 10.1021/jm970527v.
9
Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.4-[(氨基磺酰基)氧基]苯甲酸的烷基和环烷基酯衍生物对雌酮硫酸酯酶（ES）的抑制作用。
Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9. doi: 10.1016/j.bmcl.2003.11.067.
10
The design, synthesis, and in vitro biochemical evaluation of a series of esters of 4-[(aminosulfonyl)oxy]benzoate as novel and highly potent inhibitors of estrone sulfatase.
Biochem Biophys Res Commun. 2003 Aug 8;307(4):778-81. doi: 10.1016/s0006-291x(03)01258-0.

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验