Document Detail

Effects of the alpha-D-anomer of 5-aza-2'-deoxycytidine on L1210 mouse leukemic cells in vitro and in vivo.
MedLine Citation:
PMID:  6207913     Owner:  NLM     Status:  MEDLINE    
The alpha-D-anomer of 5-aza-2'-deoxycytidine inhibited cell growth in vitro in L1210 mouse leukemic cells (concentration causing 50% inhibition about 1 X 10(-6) M) and was also active in vivo in increasing the life span of mice with L1210 leukemia by 100% after a single i.p. injection (800 to 1000 mg/kg). This effect could be reversed by 2'-deoxycytidine. The alpha-D-anomer produced approximately 100-fold less host toxicity than did 5-aza-2'-deoxycytidine. It was observed that alpha-D-anomer, when kept at 23 degrees for 72 hr, inhibited the uptake of radioactive 2'-deoxycytidine by L1210 cells in vitro as well as the phosphorylation of 2'-deoxycytidine by a cell-free extract from L1210 cells. These effects could not be obtained with the fresh solution of the drug. It is proposed that the action of alpha-D-anomer is due to its conversion to 5-aza-2'-deoxycytidine as shown by high-performance liquid chromatography performed on water solutions of both anomers.
J Veselý; A Pískala
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Cancer research     Volume:  44     ISSN:  0008-5472     ISO Abbreviation:  Cancer Res.     Publication Date:  1984 Nov 
Date Detail:
Created Date:  1984-11-28     Completed Date:  1984-11-28     Revised Date:  2013-06-03    
Medline Journal Info:
Nlm Unique ID:  2984705R     Medline TA:  Cancer Res     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  5165-8     Citation Subset:  IM    
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MeSH Terms
Azacitidine / analogs & derivatives*,  therapeutic use,  toxicity
Cell Division / drug effects
DNA Replication / drug effects
Deoxycytidine Kinase / metabolism
Drug Evaluation, Preclinical
Leukemia L1210 / drug therapy*,  pathology
Transcription, Genetic / drug effects
Reg. No./Substance:
320-67-2/Azacitidine; 776B62CQ27/decitabine; EC Kinase

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

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