Synthesis and antitumor activity of 1,8-diaminoanthraquinone derivatives

Hsu Shan Huang, Hui F. Chiu, Wei Chih Lu, Chun Lung Yuan

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

Continuing our ongoing studies on cytotoxic substances, a series of regioisomeric disubstituted aminoanthraquinone (DAAQ) derivatives have been synthesized as cytotoxic activity based on a proposed bioactive amino conformation. To assess the biological activity of amino-substitution in the side-chains of anthraquinone located at positions 1 and 8 of the anthraquinone ring system. The aim of the study was to determine if members of the anthraquinone family could be used as adjuncts to increase the growth inhibiting effect of anticancer agents in rat glioma C6 cells, human hepatoma G2 cells and 2.2.15 cells. In vitro cytotoxicity data is reported for the compounds and some indications of structure-activity relationships have been discerned. A number of compounds were found to have good cytotoxicity against proliferation in these three cell lines. This has led to the discovery some of the DAAQ as a conformationally constrained structure possessing anticancer properties that displays cytotoxicity for these above cell lines and is being investigated further.

Original languageEnglish
Pages (from-to)1136-1139
Number of pages4
JournalChemical and Pharmaceutical Bulletin
Volume53
Issue number9
DOIs
Publication statusPublished - Sep 2005
Externally publishedYes

Fingerprint

Anthraquinones
Cytotoxicity
Derivatives
Cells
Cell Line
Structure-Activity Relationship
Bioactivity
Glioma
Antineoplastic Agents
Conformations
Rats
Hepatocellular Carcinoma
Substitution reactions
Growth
1,8-diaminoanthraquinone

Keywords

  • 2.2.15 cell
  • Aminoanthraquinone
  • Anthraquinone
  • Cytotoxicity
  • Human hepatoma G2 cell
  • Rat glioma C6 cell

ASJC Scopus subject areas

  • Chemistry(all)
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

Cite this

Synthesis and antitumor activity of 1,8-diaminoanthraquinone derivatives. / Huang, Hsu Shan; Chiu, Hui F.; Lu, Wei Chih; Yuan, Chun Lung.

In: Chemical and Pharmaceutical Bulletin, Vol. 53, No. 9, 09.2005, p. 1136-1139.

Research output: Contribution to journalArticle

Huang, Hsu Shan ; Chiu, Hui F. ; Lu, Wei Chih ; Yuan, Chun Lung. / Synthesis and antitumor activity of 1,8-diaminoanthraquinone derivatives. In: Chemical and Pharmaceutical Bulletin. 2005 ; Vol. 53, No. 9. pp. 1136-1139.
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