Synthesis and antitumor activity of bis(arylsulfonyl)dihydroimidazolinone derivatives

Bioorg Med Chem Lett. 2020 Jan 1;30(1):126776. doi: 10.1016/j.bmcl.2019.126776. Epub 2019 Oct 28.

Abstract

A series of novel bis(arylsulfonyl)dihydroimidazolinones with different aryl substitution patterns were readily synthesized and evaluated for their antitumor activities. Some of the newly synthesized compounds exhibited cytotoxicity at micromolar range against multiple cancer cell lines, including A549, HepG2, HuCCA-1, and MOLT-3. The most potent analogue contained pentafluorobenzenesulfonyl groups, which could be chemically elaborated to serve as a potential pharmacophore.

Keywords: Antitumor; Bis(arylsulfonyl)dihydroimidazolinones; Cytotoxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Hep G2 Cells
  • Humans
  • Imidazolines / chemical synthesis*
  • Imidazolines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Imidazolines