Discovery of pyrazolone spirocyclohexadienone derivatives with potent antitumor activity

Bioorg Med Chem Lett. 2020 Jan 1;30(1):126662. doi: 10.1016/j.bmcl.2019.126662. Epub 2019 Oct 8.

Abstract

Starting from easy accessible pyrazoletetrahydropyran acetals, a series of new pyrazolone spirocyclohexadienone derivatives were synthesized and assayed for antitumor activity. Compound 10s was identified to possess good antitumor activity. It could induce MDA-MB-231 cancer cell apoptosis in a concentration dependent manner and arrest the cell cycle progression mainly at the G1 phase.

Keywords: Antitumor; Pyrazolone spirocyclohexadienone; Structure-activity relationship.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Pyrazolones / pharmacology
  • Pyrazolones / therapeutic use*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Pyrazolones