| Synthesis and Biological Evaluation of Novel Antifolate Analogs as Potential Anticancer Treatment. | |
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MedLine Citation:
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PMID: 23157590 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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Dan F Stoicescu; Maria Rotaru |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-11-13 |
Journal Detail:
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Title: Anti-cancer agents in medicinal chemistry Volume: - ISSN: 1875-5992 ISO Abbreviation: Anticancer Agents Med Chem Publication Date: 2012 Nov |
Date Detail:
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Created Date: 2012-11-19 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101265649 Medline TA: Anticancer Agents Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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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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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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