ACS Medicinal Chemistry Letters
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#1Zhuming Zhang (Janssen Pharmaceutica)H-Index: 1
#2Peter J. Connolly (Janssen Pharmaceutica)H-Index: 4
Last. Ian Hickson (Janssen Pharmaceutica)H-Index: 20
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#1Dong Huang (SYSU: Sun Yat-sen University)H-Index: 1
#2Rui-Min Wang (SYSU: Sun Yat-sen University)H-Index: 1
Last. Sheng Yin (SYSU: Sun Yat-sen University)H-Index: 17
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Pregnane X receptor (PXR) that orchestrates the intricate network of xeno- and endobiotic metabolism is considered as a promising therapeutic target for cholestasis. In this study, the human PXR (hPXR) agonistic bioassay-guided isolation of Euphorbia lathyris followed by the structural modification led to the construction of a lathyrane diterpenoid library (1-34). Subsequent assay of this library led to the identification of a series of potent hPXR agonists, showing better efficacy than that of ...
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#1Christopher M Woodley (University of Liverpool)H-Index: 1
#2Gemma L. Nixon (University of Liverpool)H-Index: 16
Last. Keiko Onuma (Eisai)
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Synthetic endoperoxide antimalarials, such as 1,2,4-trioxolanes and 1,2,4,5-tetraoxanes, are promising successors for current front-line antimalarials, semisynthetic artemisinin derivatives. However, limited solubility of second-generation analogues in biological-relevant media represents a barrier in clinical development. We present methodology for the synthesis of nonlinear analogues of second-generation tetraoxane antimalarials E209 and N205 to investigate reduced molecular symmetry on in vit...
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