The synthesis, structural study and anticancer activity evaluation of emodin derivatives containing conjugative groups

Med Chem. 2013 Jun 1;9(4):545-52. doi: 10.2174/1573406411309040008.

Abstract

Eight new emodin derivatives that contain large conjugative system have been synthesized and their anticancer activities also have been evaluated. The result shows that large conjugative system can not enhance the anticancer activities of emodin derivatives, but the introduction of an alkylating center can make emodin derivative effective against cancer cell lines. Compound 12 has the highest alkylating ability, but its anticancer activity is not remarkable, which indicates that there is not a direct correlation between the chemical reactivity of the alkylating agent and the toxic effects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents, Alkylating / chemical synthesis
  • Antineoplastic Agents, Alkylating / pharmacology
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Emodin / analogs & derivatives*
  • Emodin / chemical synthesis*
  • Emodin / pharmacology
  • Humans
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Antineoplastic Agents, Alkylating
  • Emodin