Document Detail


Synthesis and Biological Evaluation of Novel Antifolate Analogs as Potential Anticancer Treatment.
MedLine Citation:
PMID:  23157590     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
A novel process for the preparation of two ketomethylenic antifolates, 2-(2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-amino]-phenyl}-2-oxo-ethyl) pentanedioic acid and 2-(2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-methyl-amino]-phenyl}-2-oxo-ethyl) pentanedioic acid is described herein. Both compounds were compared with methotrexate as inhibitors of human dihydrofolate reductase and thymidylate synthase. The in-vitro and in-vivo results suggest that these novel antifolate inhibitors could potentially constitute effective therapeutic molecules in the treatment of certain cancers and might present a lower toxicity profile than methotrexate.
Authors:
Dan F Stoicescu; Maria Rotaru
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-13
Journal Detail:
Title:  Anti-cancer agents in medicinal chemistry     Volume:  -     ISSN:  1875-5992     ISO Abbreviation:  Anticancer Agents Med Chem     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-19     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101265649     Medline TA:  Anticancer Agents Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
University of Bucharest, Faculty of Chemistry, Department of Analytical Chemistry, 90-92 Panduri St, 050663 Bucharest, Romania Turio Ltd, 81/8 Shepherds Hill, London N6 5RG, UK. office@turio.co.uk.
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