- Discovery of carbazole derivatives as novel allosteric MEK inhibitors by pharmacophore modeling and virtual screening
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We report in this work the discovery of novel allosteric MEK inhibitors by pharmacophore modeling and virtual screening. Two out of 13 virtual hit compounds were identified as MEK kinase inhibitors using a MEK1 binding assay. Structural derivations on the
- Xi, Dandan,Niu, Yan,Li, Hongyue,Noha, Stefan M.,Temml, Veronika,Schuster, Daniela,Wang, Chao,Xu, Fengrong,Xu, Ping
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p. 802 - 817
(2019/06/27)
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- With MEK kinase inhibiting compound of the function and its preparation method and application
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The invention discloses a compound with an MEK kinase inhibition function, and a preparation method and application thereof. The chemical structure of the compound is as shown in a formula I which is described in the specification. Moreover, the invention provides the preparation method for the compound. Research shows that the compound has good MEK kinase inhibition activity and has wide application values in fields related to an MEK kinases inhibitor.
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Paragraph 0117-0121
(2017/11/16)
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- Easy conjugations between molecules via copper-catalyzed reactions of ortho-aromatic diamines with ketones
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It is a great challenge to achieve a useful reaction under benign conditions. In this paper, a highly efficient method for copper-catalyzed conjugations of o-aromatic diamines with ketones has been developed using benign chemistry. Interestingly, the conjugation between the biological small molecules worked very well.
- Lu, Juyou,Yang, Haijun,Jin, Yunhe,Jiang, Yuyang,Fu, Hua
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p. 3184 - 3187
(2013/11/06)
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- BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT
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The present invention is directed to methods of treating diseases or conditions mediated by elevated persistent sodium channel, such as ocular disorders, pain, multiple sclerosis, and seizure disorders utilizing a compound of Formula I or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising said compound, wherein variables R, R1, R2, R3, R4, R5, m, and n in Formula I are as defined herein
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Page/Page column 35
(2013/07/19)
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- Synthesis and biological activity of novel 1,2-disubstituted benzene derivatives as factor Xa inhibitors
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Factor Xa (fXa) is a serine protease that plays a pivotal role in the coagulation cascade. High-throughput screening of the Yamanouchi compound library yielded lead compound 1 with the ability to inhibit fXa at micromolar concentrations. To improve its fX
- Koshio, Hiroyuki,Hirayama, Fukushi,Ishihara, Tsukasa,Shiraki, Ryouta,Shigenaga, Takeshi,Taniuchi, Yuta,Sato, Kazuo,Moritani, Yumiko,Iwatsuki, Yoshiyuki,Kaku, Seiji,Katayama, Naoko,Kawasaki, Tomihisa,Matsumoto, Yuzo,Sakamoto, Shuichi,Tsukamoto, Shin-Ichi
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p. 1305 - 1323
(2007/10/03)
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