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Antiproliferative activity of derivatives of trans-bis(salicylaldoximato)copper(II) in vitro. Some in vivo properties of the parent compound.

Abstract
Several derivatives and analogs of the recently reported antiproliferative and antitumor agent trans-bis(salicylaldoximato)copper(II) (CuSAO2) have been prepared and tested for antiproliferative activity against L1210 leukemia cells in vitro. The salicylaldimine analog of CuSAO2 had a very strong antiproliferative activity, the 2-day IC50 value being lower than 3 micrograms/ml. The 2,3-dihydroxybenzaldoxime analog was equally active with CuSAO2, while the corresponding 2,5-dihydroxy derivative had a slightly lower activity. The 2,3,4-trihydroxybenzaldoxime derivative had a much lower activity than had the dihydroxybenzaldoxime derivatives. The zinc(II) analog of CuSAO2 had only a low antiproliferative activity. The ligand of CuSAO2, salicylaldoxime, resembles pyridoxal oxime, a vitamin B6 antagonist and a powerful inhibitor of pyridoxal kinase. An attempt to reduce the toxicity of CuSAO2 in vivo with pyridoxal hydrochloride led to increased toxicity.
AuthorsH Elo, P Lumme
JournalZeitschrift fur Naturforschung. C, Journal of biosciences (Z Naturforsch C J Biosci) 1986 Sep-Oct Vol. 41 Issue 9-10 Pg. 951-5 ISSN: 0939-5075 [Print] Germany
PMID2948333 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Organometallic Compounds
  • bis(salicylaldoximato)copper(II)
  • Copper
  • Zinc
Topics
  • Animals
  • Body Weight (drug effects)
  • Cell Survival (drug effects)
  • Copper (therapeutic use, toxicity)
  • Leukemia L1210 (drug therapy, pathology)
  • Mice
  • Mice, Inbred Strains
  • Organometallic Compounds (therapeutic use, toxicity)
  • Structure-Activity Relationship
  • Zinc (therapeutic use, toxicity)

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