Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening

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16 Citazioni (Scopus)

Abstract

The design through energy-based pharmacophore virtual screening has led to aminocyanopyridine derivatives as efficacious new inhibitors of Hsp90. The synthesized compounds showed a good affinity for the Hsp90 ATP binding site in the competitive binding assay. Moreover, they showed an excellent antiproliferative activity against a large number of human tumor cell lines. Further biological studies on the derivative with the higher EC50 confirmed its specific influence on the cellular pathways involving Hsp90.
Lingua originaleEnglish
pagine (da-a)3424-3428
Numero di pagine5
RivistaJournal of Medicinal Chemistry
Volume56
Stato di pubblicazionePublished - 2013

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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