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Inhibition of mammalian tumour thymidylate synthetase by 5-alkylated 2'-deoxyuridine 5'-phosphates.

Abstract：

:Improved syntheses, based on Lewis acid-catalyzed nucleosidation, are described for the preparation of 5-alkyl-2'-deoxyuridines. These were converted to their 5'-phosphates with the use of wheat shoot phosphotransferase. The dUMP analogues, 5-ethyl-dUMP and 5-propyl-dUMP, were competitive vs dUMP inhibitors of thymidylate synthetase purified from mouse L1210, Ehrlich ascites and HeLa cells, the former being the stronger inhibitor. Both analogues were shown to bind cooperatively to each of the mouse tumour enzymes, two molecules of inhibitor interacting with a single enzyme molecule, as reflected by the parabolic character of the replots of the slope vs inhibitor concentrations. dTMP was a stronger inhibitor of the mouse tumour enzymes than its higher alkyl homologues.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Rode W,Kulikowski T,Kedzierska B,Jastreboff M,Shugar D

doi

10.1016/0006-2952(84)90683-x

subject

Has Abstract

pub_date

1984-09-01 00:00:00

pages

2699-705

issue

17

eissn

0006-2952

issn

1873-2968

pii

0006-2952(84)90683-X

journal_volume

33

pub_type

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