- Preparation method and application of selective butyryl cholinesterase inhibitor. (by machine translation)
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The invention discloses a preparation method and application (I) of the selective butyryl cholinesterase inhibitor, with the general formula. to evaluate the selectivity of cholinesterase inhibition activity, to find that it has good in-vitro activity and
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Paragraph 0048-0050
(2020/03/12)
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- Development of thieno- and benzopyrimidinone inhibitors of the Hedgehog signaling pathway reveals PDE4-dependent and PDE4-independent mechanisms of action
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From a high content in vivo screen for modulators of developmental patterning in embryonic zebrafish, we previously identified eggmanone (EGM1, 3) as a Hedgehog (Hh) signaling inhibitor functioning downstream of Smoothened. Phenotypic optimization studies for in vitro probe development utilizing a Gli transcription-linked stable luciferase reporter cell line identified EGM1 analogs with improved potency and aqueous solubility. Mechanistic profiling of optimized analogs indicated two distinct scaffold clusters: PDE4 inhibitors able to inhibit downstream of Sufu, and PDE4-independent Hh inhibitors functioning between Smo and Sufu. Each class represents valuable in vitro probes for elucidating the complex mechanisms of Hh regulation.
- Hempel, Jonathan E.,Cadar, Adrian G.,Hong, Charles C.
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supporting information
p. 1947 - 1953
(2016/04/05)
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- NOVEL COMPOUND HAVING ANGIOGENESIS INHIBITORY ACTIVITY, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formular I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent.
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Paragraph 0047; 0048; 00453; 00454
(2014/07/23)
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