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举例 :可输入Filippa Pettersson 或者 Cancer Res. 75(6) , 1102-12, (2015) 或者10.1002/anie.201600521

The first potent inhibitor of mammalian group X secreted phospholipase A2: elucidation of sites for enhanced binding

BP Smart, RC Oslund, LA Walsh…

文献索引：Smart, Brian P.; Oslund, Rob C.; Walsh, Laura A.; Gelb, Michael H. Journal of Medicinal Chemistry, 2006 , vol. 49, # 10 p. 2858 - 2860

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被引用次数: 75

摘要

Using the X-ray structure of human group X secreted phospholipase A2 (hGX), we carried out structure-based design of indole-based inhibitors and prepared the compounds using a new synthetic route. The most potent compound inhibited hGX and the mouse orthologue with an IC50 of 75 nM. This compound is the most potent hGX inhibitor reported to date and was also found to inhibit a subset of the other mouse and human sPLA2s.

4-苄氧基吲哚结构式

4-苄氧基吲哚

苯磺酰氯结构式

~81%

4-(苄氧基)-1-(苯磺酰基)-1H-吲哚结构式

4-(苄氧基)-1-(苯磺酰基...

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1-(4-phenylmeth...

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1-(4-(苄氧基)-1-(苯...

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2-乙基-4-(苯基甲氧基)-1H-吲哚

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4-苄氧基吲哚结构式

4-苄氧基吲哚

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2-乙基-4-(苯基甲氧基)-1H-吲哚结构式

2-乙基-4-(苯基甲氧基)-1H-吲哚

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溴化苄结构式

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2-乙基-4-(苯基甲氧基)-1H-吲哚结构式

2-乙基-4-(苯基甲氧基)-1H-吲哚

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4-(苄氧基)-1-(苯磺酰基)-1H-吲哚结构式

4-(苄氧基)-1-(苯磺酰基...

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2-乙基-4-(苯基甲氧基)-1H-吲哚结构式

2-乙基-4-(苯基甲氧基)-1H-吲哚

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2-乙基-4-(苯基甲氧基)-1H-吲哚结构式

2-乙基-4-(苯基甲氧基)-1H-吲哚

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2-(3-(2-氨基-2-氧代乙酰基)-1-苄基-2-乙基-1H-吲哚-4-基氧基)乙酸叔丁酯结构式

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1-(4-(苄氧基)-1-(苯...

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4-苄氧基吲哚结构式

4-苄氧基吲哚

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2-(3-(2-氨基-2-氧代...

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4-(苄氧基)-1-(苯磺酰基)-1H-吲哚结构式

4-(苄氧基)-1-(苯磺酰基...

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tert-butyl 2-(1...

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溴乙酸叔丁酯

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2-(3-(2-氨基-2-氧代乙酰基)-1-苄基-2-乙基-1H-吲哚-4-基氧基)乙酸叔丁酯结构式

2-(3-(2-氨基-2-氧代...

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4-(苄氧基)-1-(苯磺酰基)-1H-吲哚结构式

4-(苄氧基)-1-(苯磺酰基...

~91%

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4-苄氧基吲哚

~%

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2,6-dimethyl-1H-indol-4-ol结构式

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2,6-dimethyl-1H-indol-4-ol结构式

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6-methyl-1-(phenylsulfonyl)-1H-indol-4-ol结构式

6-methyl-1-(phe...

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The first potent inhibitor of mammalian group X secreted pho...

[Journal of Medicinal Chemistry, , vol. 49, # 10 p. 2858 - 2860]

The first potent inhibitor of mammalian group X secreted pho...

[Journal of Medicinal Chemistry, , vol. 49, # 10 p. 2858 - 2860]

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[Chemical and Pharmaceutical Bulletin, , vol. 42, # 2 p. 271 - 276]

New, Concise Route to Indoles Bearing Oxygen or Sulfur Subst...

[Chemical and Pharmaceutical Bulletin, , vol. 42, # 2 p. 271 - 276]