Synthesis, DNA binding and cytotoxicity of new pyrazole emodin derivatives

J. H. Tan, Q. X. Zhang, Z. S. Huang, Y. Chen, X. D. Wang, L. Q. Gu, Jianyong Wu

Research output: Journal article publicationJournal articleAcademic researchpeer-review

46 Citations (Scopus)

Abstract

A series of new anthrapyrazoles were derived from emodin by attaching various cationic alkyl amino side chains onto a pyrazole ring which had been incorporated into the anthraquinone chromophore. Compared with emodin, the derivatives had significantly higher DNA binding affinity based on interaction with calf thymus DNA, and much more potent cytotoxicity against different tumor cells. The derivatives with a mono-cationic alkyl side chain exhibited the highest DNA binding affinity and cytotoxicity.
Original languageEnglish
Pages (from-to)1041-1047
Number of pages7
JournalEuropean Journal of Medicinal Chemistry
Volume41
Issue number9
DOIs
Publication statusPublished - 1 Sep 2006

Keywords

  • Amino side chain
  • Anthrapyrazole
  • Cytotoxicity
  • DNA binding
  • Emodin derivatives
  • Tumor cells

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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