New cyclopentane derivatives as inhibitors of steroid metabolizing enzymes AKR1C1 and AKR1C3.

Brozic Petra; Vehovc Matej; Rizner Tea Lanisnik; Gobec Stanislav

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New cyclopentane derivatives as inhibitors of steroid metabolizing enzymes AKR1C1 and AKR1C3.

机译：新的环戊烷衍生物作为类固醇代谢酶AKR1C1和AKR1C3的抑制剂。

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A series of cyclopentane derivatives was synthesized and evaluated for inhibition of the steroid metabolizing enzymes AKR1C1 and AKR1C3. Selective inhibitors that are active in the low micromolar range were identified. These compounds represent promising starting points in the development of new anticancer agents for the treatment of hormone-dependent forms of cancer and other diseases where AKR1C1 and AKR1C3 are involved.

机译：合成了一系列环戊烷衍生物，并评估了其对类固醇代谢酶AKR1C1和AKR1C3的抑制作用。鉴定了在低微摩尔范围内有活性的选择性抑制剂。这些化合物代表了开发新的抗癌药物的有前途的起点，这些新的抗癌药物用于治疗激素依赖性形式的癌症和涉及AKR1C1和AKR1C3的其他疾病。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2009年第6期|共9页
作者
Brozic Petra; Vehovc Matej; Rizner Tea Lanisnik; Gobec Stanislav;
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正文语种 eng
中图分类药学;
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1. New cyclopentane derivatives as inhibitors of steroid metabolizing enzymes AKR1C1 and AKR1C3. [J] . Brozic Petra, Vehovc Matej, Rizner Tea Lanisnik, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第6期

机译：新的环戊烷衍生物作为类固醇代谢酶AKR1C1和AKR1C3的抑制剂。
2. Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives [J] . Sahin Zafer, Ertas Merve, Berk Barkin, Bioorganic and medicinal chemistry . 2018,第8期

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3. Activity of steroid 4 and derivatives 4a–4f as inhibitors of the enzyme 5α-reductase 1 [J] . Yazmín Arellano, Eugene Bratoeff, Yvonne Heuze, Bioorganic and medicinal chemistry . 2018,第14期

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4. Effects of L-Arabinose on Drug Metabolizing and Antioxidant Enzymes in Rat [C] . Ziming Yang, Li Zhang, Yueyuan Chen, International Conference on Advanced Design and Manufacturing Engineering . 2016

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6. Design synthesis and biological evaluation of new arylamide derivatives possessing sulfonate or sulfamate moieties as steroid sulfatase enzyme inhibitors [O] . Mohammed I. El-Gamal, Mohammad H. Semreen, Paul A. Foster, -1

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New cyclopentane derivatives as inhibitors of steroid metabolizing enzymes AKR1C1 and AKR1C3.

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