Synthesis of β-boswellic acid derivatives as cytotoxic and apoptotic agents

Bioorg Med Chem Lett. 2016 Jan 1;26(1):76-81. doi: 10.1016/j.bmcl.2015.11.027. Epub 2015 Nov 11.

Abstract

A series of β-boswellic acid derivatives were synthesized and evaluated for anticancer activity. One of the lead analog 4f displayed significant anticancer activity against a panel of cancer cells as well as substantially inhibited colony formation in HCT-116 cells. Furthermore, 4f was found to be a potent inducer of apoptosis confirmed by loss of mitochondrial membrane potential, DAPI staining, Western blotting and ROS generation.

Keywords: Anticancer; Apoptosis; Triterpenoid; β-Boswellic acid.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • HCT116 Cells
  • Humans
  • Molecular Conformation
  • Structure-Activity Relationship
  • Triterpenes / chemical synthesis
  • Triterpenes / chemistry*
  • Triterpenes / pharmacology*

Substances

  • Antineoplastic Agents
  • Triterpenes
  • boswellic acid