Suppr超能文献

新型肉桂基三唑类化合物作为强效和选择性芳香化酶（细胞色素P450 19A1）抑制剂的发现。

Discovery of a new class of cinnamyl-triazole as potent and selective inhibitors of aromatase (cytochrome P450 19A1).

作者信息

McNulty James, Keskar Kunal, Crankshaw Denis J, Holloway Alison C

机构信息

Department of Chemistry and Chemical Biology, McMaster University, 1280 Main Street West, Hamilton, Ont. L8S 4M1, Canada.

Department of Obstetrics and Gynecology, McMaster University, 1280 Main Street West, Hamilton, Ont. L8S 4K1, Canada.

出版信息

Bioorg Med Chem Lett. 2014 Sep 15;24(18):4586-4589. doi: 10.1016/j.bmcl.2014.07.083. Epub 2014 Aug 7.

DOI:10.1016/j.bmcl.2014.07.083
PMID:25155384
Abstract

Synthesis of a novel class of natural product inspired cinnamyl-containing 1,4,5-triazole and the potent inhibition of human aromatase (CYP 450 19A1) by select members is described. Structure-activity data generated provides insights into the requirements for potency particularly the inclusion of an aryl bromide or chloride residue as a keto-bioisostere.

摘要

描述了一类受天然产物启发的新型含肉桂基1,4,5-三唑的合成，以及部分成员对人芳香酶（CYP 450 19A1）的强效抑制作用。所产生的构效关系数据为药效的要求提供了见解，特别是作为酮生物电子等排体的芳基溴或氯残基的引入。

相似文献

1
Discovery of a new class of cinnamyl-triazole as potent and selective inhibitors of aromatase (cytochrome P450 19A1).
Bioorg Med Chem Lett. 2014 Sep 15;24(18):4586-4589. doi: 10.1016/j.bmcl.2014.07.083. Epub 2014 Aug 7.
2
Discovery of a novel class of aldol-derived 1,2,3-triazoles: potent and selective inhibitors of human cytochrome P450 19A1 (aromatase).
Bioorg Med Chem Lett. 2012 Jan 1;22(1):718-22. doi: 10.1016/j.bmcl.2011.10.039. Epub 2011 Oct 20.
3
Investigation of aryl halides as ketone bioisosteres: refinement of potent and selective inhibitors of human cytochrome P450 19A1 (aromatase).
Bioorg Med Chem Lett. 2013 Nov 15;23(22):6060-3. doi: 10.1016/j.bmcl.2013.09.030. Epub 2013 Sep 18.
4
Synthesis of α-methylstilbenes using an aqueous Wittig methodology and application toward the development of potent human aromatase inhibitors.
Bioorg Med Chem Lett. 2019 Jun 1;29(11):1395-1398. doi: 10.1016/j.bmcl.2019.03.033. Epub 2019 Mar 26.
5
Synthesis and aromatase inhibitory evaluation of 4-N-nitrophenyl substituted amino-4H-1,2,4-triazole derivatives.
Bioorg Med Chem. 2016 Oct 1;24(19):4723-4730. doi: 10.1016/j.bmc.2016.08.014. Epub 2016 Aug 10.
6
QSAR modeling of aromatase inhibitory activity of 1-substituted 1,2,3-triazole analogs of letrozole.
Eur J Med Chem. 2013 Nov;69:99-114. doi: 10.1016/j.ejmech.2013.08.015. Epub 2013 Aug 19.
7
Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors.
Bioorg Chem. 2019 Dec;93:103327. doi: 10.1016/j.bioorg.2019.103327. Epub 2019 Sep 28.
8
Design and Pharmacophore Study of Triazole Analogues as Aromatase Inhibitors.
Anticancer Agents Med Chem. 2024;24(4):288-303. doi: 10.2174/0118715206265278231026101739.
9
Synthesis and structure-activity relationship of 1- and 2-substituted-1,2,3-triazole letrozole-based analogues as aromatase inhibitors.
Eur J Med Chem. 2011 Sep;46(9):4010-24. doi: 10.1016/j.ejmech.2011.05.074. Epub 2011 Jun 12.
10
Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
Bioorg Med Chem Lett. 2004 Oct 18;14(20):5215-8. doi: 10.1016/j.bmcl.2004.07.090.

引用本文的文献

1
Aromatase Inhibitors as a Promising Direction for the Search for New Anticancer Drugs.
Molecules. 2024 Jan 10;29(2):346. doi: 10.3390/molecules29020346.
2
Human cytochrome P450 enzymes 5-51 as targets of drugs and natural and environmental compounds: mechanisms, induction, and inhibition - toxic effects and benefits.
Drug Metab Rev. 2018 Aug;50(3):256-342. doi: 10.1080/03602532.2018.1483401.

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型，支持多种主流文档格式。

立即体验