Document Detail

Comparative analysis of the cytotoxicity of substituted (phenylglyoxal bis(4-methyl-3-thiosemicarbazone)) copper (II) chelates.
MedLine Citation:
PMID:  1246035     Owner:  NLM     Status:  MEDLINE    
Seven para-substituted [phenylglyoxal bis(4-methyl-3-thiosemicarbazone)]copper (II) chelates (12-18) have been designed, synthesized, and tested for their ability to inhibit the respiration of rat liver slices as a normal cell model and Ehrlich ascites cells as a tumor cell model. Relationships between chemical structure and respiratory inhibition are described on a quantitative basis using substituent contants (pi, Es, and sigmap) by computerized multiparameter regression analyses. The correlations indicate that changes in Es have the largest effect on liver slice toxicity of chelates while pi and sigmap account for most of the variation in toxicity to ascites cells. A comparative analysis strongly suggests that electron-donating substituents with greater water solubility should increase cytotoxicity to ascites cells at the expense of cytotoxicity to the rat liver cells. The predictions of the equations were checked by synthesizing and testing an additional derivative. The results strengthen the initial predictions.
E A Coats; S R Milstein; G Holbein; J McDonald; R Reed; H G Petering
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Publication Detail:
Type:  Comparative Study; In Vitro; Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  19     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  1976 Jan 
Date Detail:
Created Date:  1976-03-24     Completed Date:  1976-03-24     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  131-5     Citation Subset:  IM    
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MeSH Terms
Antineoplastic Agents / chemical synthesis*,  pharmacology
Carcinoma, Ehrlich Tumor / metabolism
Chelating Agents
Copper* / pharmacology
Liver / metabolism
Oxygen Consumption / drug effects
Regression Analysis
Spectrophotometry, Ultraviolet
Structure-Activity Relationship
Thiosemicarbazones / chemical synthesis*,  pharmacology
Reg. No./Substance:
0/Antineoplastic Agents; 0/Chelating Agents; 0/Thiosemicarbazones; 7440-50-8/Copper

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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