Synthesis of Constrained Heterocycles Employing Two Post-Ugi Cyclization Methods for Rapid Library Generation with In Cellulo Activity

Nicholas McConnell, Zhigang Xu, Vishnu Kumarasamy, Daekyu Sun, Brendan Frett, Hong Yu Li

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

Benzimidazoles and quinoxalinones are present in the core of many pharmacologically relevant compounds. Several combinatorial methods have been developed to attach ring systems to both scaffolds for derivatization at select positions. Herein, we describe the development of novel constrained heterocyclic compounds attached to the N1 position of both benzimidazole and quinoxalinone scaffolds. Utilizing robust post-Ugi cyclization methods, including the Ugi-deprotection-cyclization (UDC) methodology, allows for efficient access to a new area of chemical space. Additionally, molecular modeling and in cellulo screening was employed to therapeutically validate the compounds formed with this method.

Original languageEnglish (US)
Pages (from-to)11821-11825
Number of pages5
JournalChemistrySelect
Volume2
Issue number35
DOIs
StatePublished - Jan 1 2017

Keywords

  • Heterocycle Formation
  • MDM2/MDMX
  • Multicomponent Reaction
  • Post-Ugi Modifications
  • Ugi Condensation

ASJC Scopus subject areas

  • Chemistry(all)

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