Comparative analysis of the cytotoxicity of substituted [phenylglyoxal bis(4-methyl-3-thiosemicarbazone)]copper(II) chelates. 2. Parabolic correlations and their implications for selective toxicity
- 1 August 1978
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 21 (8) , 804-809
- https://doi.org/10.1021/jm00206a017
Abstract
An extended series of para-substituted [phenylglyoxal bis(4-methyl-3-thiosemicarbazone)]copper(II) chelates was synthesized. Biological evaluation and regression analysis was performed, correlating pI50 [the negative logarithm of the molar concentration giving 50% inhibition] with extrathermodynamic substituent parameters. Parabolic correlations with .pi. [Hansch hydrophobic substituent constant] resulted, which predict optimum lipophilic character of the para substituent with respect to [mouse] Ehrlich ascites cytotoxicity (.pi.o = 2.13) and with respect to [mouse] ascites vs. [rat] liver slice cytotoxicity (.pi.o = -1.31). The chelate most toxic to the tumor cell model may not be the most selective.This publication has 3 references indexed in Scilit:
- Platinum complexes: A new class of antineoplastic agentsJournal of Pharmaceutical Sciences, 1976
- Sites of Inhibition of DNA Synthesis by Kethoxal bis(Thiosemicarbazone)Nature, 1968
- INHIBITION OF GROWTH OF SARCOMA 180 ASCITES CELLS BY COMBINATIONS OF INHIBITORS OF NUCLEIC ACID BIOSYNTHESIS AND CUPRIC CHELATE OF KETHOXAL BIS-(THIOSEMICARBAZONE)1967