Identification and Mechanistic Studies of a Cell Cycle Regulator JP18 from a Library of Synthetic Indole Terpenoid Mimics

Chem Asian J. 2016 Oct 6;11(19):2715-2718. doi: 10.1002/asia.201600714. Epub 2016 Aug 2.

Abstract

We constructed a small library of indole terpenoid mimics using a hybridizing strategy to link various indole and α,β-unsaturated enone building blocks together. Prepared compounds were evaluated for the cytotoxicity against a panel of cancer cell lines. An indolyl ketone called JP18 was identified as a cell cycle regulator, and the underlying mechanism was investigated.

Keywords: CDK/cyclin complexes; cell cycle arrest; hybrid structures; indoles; terpenoids.

MeSH terms

  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cyclin-Dependent Kinases / chemistry
  • Cyclin-Dependent Kinases / metabolism
  • Cyclins / chemistry
  • Cyclins / metabolism
  • G2 Phase Cell Cycle Checkpoints / drug effects
  • Humans
  • Indoles / chemistry*
  • Ketones / chemistry*
  • Ketones / toxicity
  • M Phase Cell Cycle Checkpoints / drug effects
  • Terpenes / chemistry*
  • Terpenes / toxicity

Substances

  • Cyclins
  • Indoles
  • Ketones
  • Terpenes
  • indole
  • Cyclin-Dependent Kinases