Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme

Gobbi S; Cavalli A; Rampa A; Belluti F; Piazzi L; Paluszcak A; Hartmann RW; Recanatini M; Bisi A

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Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme

机译：领先的优化技术，提供了一系列黄酮衍生物，作为细胞色素P450芳香化酶的有效非甾体抑制剂

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Following our SAR studies on aromatase inhibitors, new compounds were designed by appropriately modifying the structure of flavone 1 using our previously reported CoMFA model. While the introduction of substituents on the 2-phenyl ring alone did not cause improvement in potency, these modifications and the removal of the 7-methoxy group led to compounds showing inhibitory activity in the nanomolar range, comparable to the marketed drug fadrozole.

机译：在我们对芳香酶抑制剂的SAR研究之后，使用我们先前报道的CoMFA模型，通过适当修饰黄酮1的结构来设计新化合物。尽管仅在2-苯环上引入取代基并不能提高效能，但是这些修饰和7-甲氧基的去除导致化合物在纳摩尔范围内表现出抑制活性，与市售药物法得唑相当。

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《Journal of Medicinal Chemistry》 |2006年第15期|共4页
作者
Gobbi S; Cavalli A; Rampa A; Belluti F; Piazzi L; Paluszcak A; Hartmann RW; Recanatini M; Bisi A;
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正文语种 eng
中图分类药学;
关键词
MOLECULAR-FIELD ANALYSIS; BREAST-CANCER; DESIGN; CELLS;

机译：分子电场分析;乳腺癌;设计;细胞;

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1. Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme [J] . Gobbi S, Cavalli A, Rampa A, Journal of Medicinal Chemistry . 2006,第15期

机译：领先的优化技术，提供了一系列黄酮衍生物，作为细胞色素P450芳香化酶的有效非甾体抑制剂
2. Development of Flavone Propargyl Ethers as Potent and Selective Inhibitors of Cytochrome P450 Enzymes 1A1 and 1A2. [J] . Jayalakshmi Sridhar, Jamie Ellis, Patrick Dupart, Drug metabolism letters . 2012,第4期

机译：黄酮炔丙基醚作为细胞色素P450酶1A1和1A2的强效和选择性抑制剂的发展。
3. In Vivo Active Aldosterone Synthase Inhibitors with Improved Selectivity: Lead Optimization Providing a Series of Pyridine Substituted 3,4-Dihydro-1H-quinolin-2-one Derivatives [J] . Lucas S, Heim R, Ries C, Journal of Medicinal Chemistry . 2008,第24期

机译：具有改善的选择性的体内活性Aldosterone合酶抑制剂：铅优化提供了一系列吡啶取代的3,4-Dihydro-1H-quinolin-2-one衍生物
4. cDNA Cloning and mRNA Expression of Cytochrome P450 Aromatases in Orange-spotted Grouper (Epinephelus coioides) [C] . ZHANG Yong, ZHANG Weimin, LIN Haoran Annual Conference for Young Scientists of China Association for Science and Technology; 20041120-23; Shanghai(CN) . 2004

机译：斑点石斑鱼（Epinephelus coioides）细胞色素P450芳香酶的cDNA克隆和mRNA表达
5. Part I. Synthesis of cytochrome P450-CAM substrate analogues towards developing cytochrome P450-CAM as an enzyme-based model system for mechanistic studies of important types of P450 reactions. Part II. Diels-Alder approach towards the synthesis of 2,3-disubstituted anthracene derivatives for luminescence spectroscopy characterization: Synthesis towards fluorescent sensors. [D] . Kemnitzer, William Edward. 1998

机译：第一部分。合成细胞色素P450-CAM底物类似物，以开发细胞色素P450-CAM作为一种基于酶的模型系统，用于重要类型P450反应的机理研究。第二部分Diels-Alder合成2,3-二取代蒽衍生物以进行发光光谱表征的方法：合成荧光传感器。
6. Development of Flavone Propargyl Ethers as Potent and Selective Inhibitors of Cytochrome P450 Enzymes 1A1 and 1A2 [O] . Jayalakshmi Sridhar, Jamie Ellis, Patrick Dupart, -1

机译：黄酮普通丙基醚的发展作为细胞色素P450酶1A1和1A2的有效和选择性抑制剂
7. Lead Optimization Providing a Series of Flavone Derivatives as Potent Nonsteroidal Inhibitors of the Cytochrome P450 Aromatase Enzyme [O] . -1

机译：铅优化提供一系列黄酮衍生物作为细胞色素P450芳香酶酶的有效的非甾体抑制剂
8. Cytochrome P450 1A1 and Aromatase (CYP19) in Cetaceans: Enzyme Expression and Relationship to Contaminant Exposure. [R] . Wilson, J. Y. 2003

机译：鲸类动物细胞色素p450 1a1和芳香酶（CYp19）：酶表达及其与污染物暴露的关系。

Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme

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