| Literature DB >> 30578036 |
Miyanou Rosales-Hurtado1, Alexandre Lebeau1, Cyril Bourouh2, Gerardo Cebrian-Torrejon1, Muriel Albalat3, Marion Jean3, Jean-Valère Naubron4, Jean-Sébastien Annicotte2, Zohra Benfodda1, Patrick Meffre5.
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.Entities:
Keywords: Absolute configuration determination; Betti reaction; Biological activity; HLM006474 enantiomers; Microwave assisted synthesis; Solvent-free reaction
Year: 2018 PMID： 30578036 DOI： 10.1016/j.bmcl.2018.12.037
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823