Biological activity evaluation and structure-activity relationships analysis of ferulic acid and caffeic acid derivatives for anticancer

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6085-8. doi: 10.1016/j.bmcl.2012.08.038. Epub 2012 Aug 16.

Abstract

The anticancer activities of alkyl esters and NO-donors of ferulic acid (FA) and caffeic acid (CA) were assessed by a high-throughout screening (HTS) method, and the structure-activity relationships were described. CA alkyl esters had better anticancer activities than FA alkyl esters with the same alkyl substituent. Mono-nitrates and phenylfuroxan nitrates were more potent than the dual nitrates. Phenylsulfonylfuroxan nitrates of FA, especially compounds 8b-8d, exhibited more potent activities in anticancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Caffeic Acids / chemical synthesis
  • Caffeic Acids / chemistry*
  • Caffeic Acids / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Coumaric Acids / chemical synthesis
  • Coumaric Acids / chemistry*
  • Coumaric Acids / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • HeLa Cells
  • High-Throughput Screening Assays
  • Humans
  • Molecular Structure
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Caffeic Acids
  • Coumaric Acids
  • ferulic acid
  • caffeic acid