Synthesis and Biological Evaluation of Novel Antifolate Analogs as Potential Anticancer Treatment

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 14, 10 Issues, 2014


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Ranking and Category:
  • 22nd of 58 in Chemistry, Medicinal
  • 85th of 202 in Oncology

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Synthesis and Biological Evaluation of Novel Antifolate Analogs as Potential Anticancer Treatment

Author(s): Dan F. Stoicescu and Maria Rotaru


Abstract

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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Article Details

Volume: 13
First Page: 1
Last Page: 1
Page Count: 1
DOI: 10.2174/18715206113139990106
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