Document Detail

Cellular pharmacology in murine and human leukemic cell lines of diaziquone (NSC 182986).
MedLine Citation:
PMID:  3971389     Owner:  NLM     Status:  MEDLINE    
We investigated the in vitro interaction with and antitumor effect on several murine and human leukemic cell lines of diaziquone (AZQ). L1210 cells accumulated AZQ from Roswell Park Memorial Institute Medium 1640 with or without newborn calf serum by a temperature-dependent and sodium azide-resistant process. AZQ inhibited, in a dose-dependent fashion, [3H]thymidine incorporation into L1210 cells, but this inhibition was slow to develop, requiring approximately 6 hr to become apparent. The minimal inhibitory concentration of AZQ for this process was 0.05 to 0.25 nmol/ml. AZQ was a much less effective inhibitor of L1210 cell [3H]uridine and [14C]valine incorporation. In suspension cultures, AZQ inhibited growth of L1210 and HL-60 cells at minimal inhibitory concentrations of 0.5 to 1 nmol/ml. In soft agar cultures, AZQ inhibited HL-60 cell cloning at minimal inhibitory concentrations of 0.1 to 0.3 nmol/ml. AZQ provoked a dose-dependent increase in oxygen consumption when added to intact L1210, HL-60, and K562 cells and was converted to an AZQ anion free radical by these cells. When the aziridine rings of AZQ were opened by acid treatment, the resulting molecule was not accumulated by L1210 cells, did not provoke O2 consumption, did not form free radicals when added to L1210 cells, and was a much less effective inhibitor of [3H]thymidine incorporation by L1210 cells than was AZQ.
M J Egorin; B M Fox; J F Spiegel; P L Gutierrez; R D Friedman; N R Bachur
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Cancer research     Volume:  45     ISSN:  0008-5472     ISO Abbreviation:  Cancer Res.     Publication Date:  1985 Mar 
Date Detail:
Created Date:  1985-03-27     Completed Date:  1985-03-27     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  2984705R     Medline TA:  Cancer Res     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  992-9     Citation Subset:  IM    
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MeSH Terms
Antineoplastic Agents / pharmacology*
Aziridines / metabolism,  pharmacology*
Azirines / pharmacology*
Carbon Radioisotopes
Cell Division / drug effects
Cell Line
Free Radicals
Leukemia / metabolism,  pathology*
Oxygen Consumption
Thymidine / metabolism
Uridine / metabolism
Grant Support
Reg. No./Substance:
0/Antineoplastic Agents; 0/Aziridines; 0/Azirines; 0/Benzoquinones; 0/Carbon Radioisotopes; 0/Free Radicals; 50-89-5/Thymidine; 57998-68-2/diaziquone; 58-96-8/Uridine

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