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4-三唑基黄烷类化合物作为新型芳香酶抑制剂的合成与评价

Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.

作者信息

Yahiaoui Samir, Pouget Christelle, Fagnere Catherine, Champavier Yves, Habrioux Gérard, Chulia Albert José

机构信息

UPRES EA 1085 Biomolécules et Cibles Cellulaires Tumorales, Faculté de Pharmacie, 2 rue du Docteur Marcland, 87025 Limoges, France.

出版信息

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5215-8. doi: 10.1016/j.bmcl.2004.07.090.

DOI:10.1016/j.bmcl.2004.07.090
PMID:15380230
Abstract

Aromatase is a target of pharmacological interest for the treatment of estrogen-dependent cancers. Azole derivatives such as letrozole or anastrozole have been developed for aromatase inhibition and are used for the treatment of breast tumors. In this paper, four 4-triazolylflavans were synthesized and were found to exhibit moderate to high inhibitory activity against aromatase.

摘要

芳香化酶是治疗雌激素依赖性癌症的药理学研究靶点。已开发出如来曲唑或阿那曲唑等唑类衍生物用于抑制芳香化酶，并用于治疗乳腺肿瘤。本文合成了四种4-三唑基黄烷，发现它们对芳香化酶表现出中度至高抑制活性。

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