Preliminary evaluation of the cytotoxicity of a series of tris-2-aminoethylamine (Tren) based hexadentate heterocyclic donor agents

Suzy V. Torti, Rong Ma, Vincent J. Venditto, Frank M. Torti, Roy P. Planalp, Martin W. Brechbiel

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

Tachpyridine is a cytotoxic metal chelator with potential anti-tumor activity. The synthesis and evaluation of a set of derivatives of the related hexadentate heterocyclic donor agents tris-2-aminoethylamine (tren) and tris[N-(2-pyridylmethylene)-2-aminoethyl]amine (trenpyr) was performed to compare their cytotoxic activity to tachpyridine in HeLa tumor cells. Methyl groups were added to the pyridyl ring of trenpyr, and the effects of alkyl group substitution on cell survival were assessed. Profound cytotoxicity was observed and IC50 data were obtained in ascending order from those compounds substituted with a methyl group at the 3-, 4-, or 5-position and lastly by the 6-methyl derivative. These results suggest that analogous derivatives with substitution at the 3-position of the pyridyl ring deserve further exploration.

Original languageEnglish
Pages (from-to)5961-5967
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume13
Issue number21
DOIs
StatePublished - Nov 1 2005

Bibliographical note

Funding Information:
This work was supported in part by grant No. DK 57781 (S.V.T.) from the National Institutes of Health. This research was supported in part by the Intramural Research Program of the NIH, National Cancer Institute, Center for Cancer Research.

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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