Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.

Fensome A; Koko M; Wrobel J; Zhang P; Zhang Z; Cohen J; Lundeen S; Rudnick K; Zhu Y; Winneker R

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Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.

机译：新型的5-芳基-1,3-二氢吲哚-2-硫酮。强效的口服活性孕激素受体激动剂。

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During the course of our studies on 3,3-disubstituted-5-aryloxindoles derived progesterone receptor (PR) antagonists we discovered that changing the amide funtionality to a thio-amide resulted in compounds displaying potent PR agonist activity. In this communication, the synthesis, structure activity relationships (SAR) and in vivo activity of various 5-arylthio-oxindoles will be discussed.

机译：在我们对3,3-二取代-5-芳基氧吲哚衍生的孕激素受体（PR）拮抗剂的研究过程中，我们发现将酰胺官能团改变为硫代酰胺会导致化合物显示出强大的PR激动剂活性。在此交流中，将讨论各种5-芳硫基-羟吲哚的合成，结构活性关系（SAR）和体内活性。

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《Bioorganic and Medicinal Chemistry Letters》 |2003年第7期|共4页
作者
Fensome A; Koko M; Wrobel J; Zhang P; Zhang Z; Cohen J; Lundeen S; Rudnick K; Zhu Y; Winneker R;
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正文语种 eng
中图分类药学;生物化学;
关键词
Receptors; Progesterone; Principal diagnosis; agonists; Thiones; 受体; 孕酮; 硫酮类;

机译：Receptors;Progesterone;Principal diagnosis;agonists;Thiones;受体;孕酮;硫酮类;

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1. Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists. [J] . Fensome A, Koko M, Wrobel J, Bioorganic and Medicinal Chemistry Letters . 2003,第7期

机译：新型的5-芳基-1,3-二氢吲哚-2-硫酮。强效的口服活性孕激素受体激动剂。
2. 5-Aryl-1,2-dihydro-5H-chromeno(3,4-f)quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents. [J] . Edwards JP, West SJ, Marschke KB, Journal of Medicinal Chemistry . 1998,第3期

机译：5-芳基-1,2-二氢-5H-铬基（3,4-f）喹啉作为有效的，口服活性的非甾体孕酮受体激动剂：D环取代基的作用。
3. 5-Aryl-1,2-dihydro-5H-chromeno(3,4-f)quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents. [J] . Edwards JP, West SJ, Marschke KB, Journal of Medicinal Chemistry . 1998,第3期

机译：5-芳基-1,2-二氢-5H-铬基（3,4-f）喹啉作为有效的，口服活性的非甾体孕酮受体激动剂：D环取代基的作用。
4. Synthesis and in vitro Pharmacological Profile of Potent and Selective Peptidic V1a Receptor Agonists. [C] . Kazinlierz Wisniewski, Robert Galyean, Hiroe Taki American Peptide Symposium . 2009

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6. Novel orally active selective progesterone receptor modulator CP8947 inhibits leiomyoma cell proliferation without adversely affecting endometrium or myometrium [O] . William H. Catherino, Minnie Malik, Paul Driggers, -1

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Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.

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