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.
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Authors | H Elo, P Lumme |
Journal | Zeitschrift 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 |
PMID | 2948333
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Organometallic Compounds
- bis(salicylaldoximato)copper(II)
- Copper
- Zinc
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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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