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