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

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


Volume 16, 12 Issues, 2016


Download PDF Flyer




Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 27th of 59 in Chemistry, Medicinal

Submit Abstracts Online Submit Manuscripts Online

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


View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.722
5 - Year: 2.849

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



Anti-Cancer Agents in Medicinal Chemistry, 13(2): 364-372.

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

Affiliation: Turio Ltd, 81/8 Shepherds Hill, London N6 5RG, UK.

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.

Keywords:

Antifolate inhibitors, Antitumor activity, Cancer therapy, Classic antifolates, Dihydrofolate reductase, Folyl polyglutamate synthetase, Chemical synthesis, Leukemia, Methotrexate, Multitarget antifolate, Non-classic antifolates, Polyglutamates, Thymidylate synthase, Tumor resistance, 2-(2-4-[(2, 4-diamino-pteridin-6-ylmethyl)-amino]-phenyl-2-oxo-ethyl) pentanedioic acid, 2-(2-4-[(2, 4-diamino-pteridin-6-ylmethyl)-methyl-amino]-phenyl-2-oxo-ethyl) pentanedioic acid.



Purchase Online Order Reprints Order Eprints Rights and Permissions




Article Details

Volume: 13
Issue Number: 2
First Page: 364
Last Page: 372
Page Count: 9
DOI: 10.2174/1871520611313020022
Price: $58
Advertisement

Related Journals




Webmaster Contact: urooj@benthamscience.org Copyright © 2016 Bentham Science