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Improved Synthesis, Resolution, Absolute Configuration Determination and Biological Evaluation of HLM006474 Enantiomers

Miyanou Rosales-Hurtado, Alexandre Lebeau, Cyril Bourouh, Gerardo Cebrian-Torrejon, Muriel Albalat, Marion Jean, Jean-Valère Naubron, Jean-Sébastien Annicotte, Zohra Benfodda, Patrick Meffre

Bioorg Med Chem Lett. 2019 Feb 1;29(3):380-382.

PMID: 30578036

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP353519638 HLM006474 HLM006474 353519-63-8 Price
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