Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton.

Nakagawa A; Uno S; Makishima M; Miyachi H; Hashimoto Y

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Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton.

机译：具有3-苯基喹唑啉-2,4-二酮/ 2-苯基异喹啉-1,3-二酮骨架的孕酮受体拮抗剂。

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摘要

Novel non-steroidal progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton were developed and their structure-activity relationships were investigated. Among the prepared compounds, 4-(4,4-diethyl-3,4-dihydro-1,3-dioxoquinolin-2(1H)-yl)benzonitrile (DEPIQ-4CN) showed the most potent activity, with IC(50) values of 74-78nM in alkaline phosphatase activity and reporter gene assays.

机译：开发了具有3-苯基喹唑啉-2,4-二酮/ 2-苯基异喹啉-1,3-二酮骨架的新型非甾体孕酮受体拮抗剂，并研究了它们的构效关系。在制备的化合物中，4-（4,4-二乙基-3,4-二氢-1,3-二氧代喹啉-2（1H）-基）苄腈（DEPIQ-4CN）表现出最强的活性，IC（50）碱性磷酸酶活性的74-78nM值和报告基因检测。

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《Bioorganic and medicinal chemistry》 |2008年第14期|共9页
作者
Nakagawa A; Uno S; Makishima M; Miyachi H; Hashimoto Y;
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正文语种 eng
中图分类药学;生物化学;
关键词
Alkaline Phosphatase; Animals; CHO Cells; Cell Line; Tumor; Cricetinae; Cricetulus; 碱性磷酸酶; 动物; CHO细胞; 仓鼠属; 基因; 报告; 半数抑制浓度; 喹唑啉类; 喹啉类;

机译：Alkaline Phosphatase;Animals;CHO Cells;Cell Line;Tumor;Cricetinae;Cricetulus;碱性磷酸酶;动物;CHO细胞;仓鼠属;基因;报告;半数抑制浓度;喹唑啉类;喹啉类;

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1. Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton. [J] . Nakagawa A, Uno S, Makishima M, Bioorganic and medicinal chemistry . 2008,第14期

机译：具有3-苯基喹唑啉-2,4-二酮/ 2-苯基异喹啉-1,3-二酮骨架的孕酮受体拮抗剂。
2. New Pyrrolo[2,l-f]purine-2,4-dione and Imidazo[2,l-f]purine-2,4-dione Derivatives as Potent and Selective Human AS Adenosine Receptor Antagonists [J] . Pier Giovanni Baraldi, Delia Preti, Mojgan Aghazadeh Tabrizi, Journal of Medicinal Chemistry . 2005,第14期

机译：新型吡咯并[2,1-f]嘌呤-2,4-二酮和咪唑并[2,1-f]嘌呤-2,4-二酮衍生物作为有效的和选择性的人类AS腺苷受体拮抗剂
3. Triterpenes from Alisma orientalis act as androgen receptor agonists, progesterone receptor antagonists, and glucocorticoid receptor antagonists [J] . LinH.-R. Bioorganic and Medicinal Chemistry Letters . 2014,第15期

机译：东方泽泻的三萜类化合物可作为雄激素受体激动剂，孕激素受体拮抗剂和糖皮质激素受体拮抗剂
4. High Progesterone Levels on the Day of hCG Administration in Controlled Ovarian Hyperstimulation Procedures Reduce the Expression of Progesterone Receptors in the Endometrium Macaca nemestrina [C] . Nurhuda, Rosalina Thuffi, Dwi Ari Pudjianto, International Symposium of Biomedical Engineering . 2019

机译：在受控卵巢过度刺激手术中HCG给药当天的高孕酮水平降低了胚胎麦卡纳涅什蒂纳内膜中黄体酮受体的表达
5. Modulation of folate receptor-alpha by glucocorticoid receptor and progesterone receptor. [D] . Tran, Thuyet Van. 2005

机译：糖皮质激素受体和孕激素受体对叶酸受体-α的调节。
6. Progesterone receptor antagonists reverse stem cell expansion and the paracrine effectors of progesterone action in the mouse mammary gland [O] . Manish Ranjan, Oukseub Lee, Gannon Cottone, 2021

机译：孕酮受体拮抗剂反向干细胞膨胀和小鼠乳腺孕酮作用的旁静脉作用
7. Antagonist-occupied human progesterone B-receptors activate transcription without binding to progesterone response elements and are dominantly inhibited by A-receptors. [O] . L Tung, M K Mohamed, J P Hoeffler, 1993

机译：拮抗剂占用的人孕酮B受体激活转录而不结合孕酮响应元件，并且由A-Proceptors占主导地位。
8. Mechanism by Which Agonist and Antagonist Occupied Progesterone Receptors Regulate Target Genes [R] . Keightley, M. C. 1998

机译：激动剂和拮抗剂占据孕酮受体调节靶基因的机制

Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton.

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