Improved synthesis, resolution, absolute configuration determination and biological evaluation of HLM006474 enantiomers

Abstract : An improved green synthesis of the E2F inhibitor HLM0066474 is described, using solvent-free and microwave irradiation conditions. The two enantiomers are separated using semi-preparative separation on Chiralpak ID and their absolute configuration is determined by vibrational circular dichroism (VCD) analysis. Biological evaluation of both enantiomers on E2F1 transcriptional activity reveals that the (+)-R, but not the (−)-S enantiomer is biologically active in repressing E2F1 transcriptional activity.
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https://hal.archives-ouvertes.fr/hal-01968387
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Submitted on : Monday, January 7, 2019 - 5:01:54 PM
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Miyanou Rosales-Hurtado, Alexandre Lebeau, Cyril Bourouh, Gerardo Cebrian-Torrejon, Muriel Albalat, et al.. Improved synthesis, resolution, absolute configuration determination and biological evaluation of HLM006474 enantiomers. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2018, ⟨10.1016/j.bmcl.2018.12.037⟩. ⟨hal-01968387⟩

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