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Synthesis and biological evaluation of some phosphate triester derivatives of the anti-cancer drug araC.

Abstract：

:A number of novel phosphate triester derivatives of the anti-cancer nucleoside analogue araC have been prepared by a rapid 2-step procedure, not necessitating prior sugar protection. Spectroscopic and lipophilicity data have been collected on these compounds. An in vitro assay indicated inhibition of thymidine incorporation by mammalian epithelial cells, by each of these compounds, in the range 3-300 microM. Moreover, the degree of inhibition showed a close correlation to chemical structure; in particular, there was a clear relationship between inhibition of thymidine incorporation and log(P). These results are consistent with cellular penetration by the intact phosphate triesters and intracellular action by an unspecified mechanism. Triethyl phosphate is inactive under the conditions of the test.

journal_name

Nucleic Acids Res

journal_title

Nucleic acids research

authors

Jones BC,McGuigan C,Riley PA

doi

10.1093/nar/17.18.7195

subject

Has Abstract

pub_date

1989-09-25 00:00:00

pages

7195-201

issue

18

eissn

0305-1048

issn

1362-4962

journal_volume

17

pub_type

杂志文章

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