Concepedia

Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (<i>S</i>)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1<i>H</i>-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)

Paul M. Wehn, James P. Rizzi, Darryl D. Dixon, Jonas Grina, Stephen T. Schlachter, Bin Wang, Rui Xu, Hanbiao Yang, Xinlin Du, Guangzhou Han,

Journal of Medicinal Chemistry · 2018 · 114 citations · 29 references

DOIFull text

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Concepts

Abstract

= 27 nM) as the clinical candidate. Finally, a retrospective crystallographic analysis describes the structural perturbations necessary for efficient antagonism.

References

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