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组蛋白赖氨酸脱甲基酶的KDM4和KDM5家族的细胞渗透抑制剂。2. Pyrido [3,4- d ]嘧啶-4（3 H）-one衍生物
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2016-01-15 00:00:00 , DOI: 10.1021/acs.jmedchem.5b01538
Susan M. Westaway 1 , Alex G. S. Preston 1 , Michael D. Barker 1 , Fiona Brown 2 , Jack A. Brown 1 , Matthew Campbell 1 , Chun-wa Chung 2 , Gerard Drewes 3 , Robert Eagle 2 , Neil Garton 1 , Laurie Gordon 2 , Carl Haslam 2 , Thomas G. Hayhow 1 , Philip G. Humphreys 1 , Gerard Joberty 3 , Roy Katso 2 , Laurens Kruidenier 1 , Melanie Leveridge 2 , Michelle Pemberton 2 , Inma Rioja 1 , Gail A. Seal 1 , Tracy Shipley 1 , Onkar Singh 2 , Colin J. Suckling 4 , Joanna Taylor 2 , Pamela Thomas 2 , David M. Wilson 1 , Kevin Lee 1 , Rab K. Prinjha 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2016-01-15 00:00:00 , DOI: 10.1021/acs.jmedchem.5b01538
Susan M. Westaway 1 , Alex G. S. Preston 1 , Michael D. Barker 1 , Fiona Brown 2 , Jack A. Brown 1 , Matthew Campbell 1 , Chun-wa Chung 2 , Gerard Drewes 3 , Robert Eagle 2 , Neil Garton 1 , Laurie Gordon 2 , Carl Haslam 2 , Thomas G. Hayhow 1 , Philip G. Humphreys 1 , Gerard Joberty 3 , Roy Katso 2 , Laurens Kruidenier 1 , Melanie Leveridge 2 , Michelle Pemberton 2 , Inma Rioja 1 , Gail A. Seal 1 , Tracy Shipley 1 , Onkar Singh 2 , Colin J. Suckling 4 , Joanna Taylor 2 , Pamela Thomas 2 , David M. Wilson 1 , Kevin Lee 1 , Rab K. Prinjha 1
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继KDM4（JMJD2）和KDM5（JARID1）组蛋白赖氨酸脱甲基酶的家族的细胞渗透剂吡啶-4-羧酸乙酯抑制剂的发现（例如，1），导致从吡啶并[3衍生的非羧酸盐抑制剂的鉴定进一步优化，4 - d ]嘧啶-4（3 H）-一。许多示例（例如化合物41）在KDM4C和KDM5C生化和靶标特异性细胞机制分析中均具有有趣的活性。
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更新日期：2016-01-15
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