Synthesis and biological evaluation of novel antifolate analogs as potential anticancer treatment.

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.

authors

Stoicescu DF,Rotaru M

doi

10.2174/1871520611313020022

subject

Has Abstract

pub_date

2013-02-01 00:00:00

pages

364-72

issue

2

eissn

1871-5206

issn

1875-5992

pii

CMCACA-EPUB-20121113-1

journal_volume

13

pub_type

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