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Synthesis and cytotoxic activity of a glucuronylated prodrug of nornitrogen mustard.

Abstract：

:A new glucuronylated prodrug of nornitrogen mustard, incorporating the same spacer group as the doxorubicin prodrug HMR 1826, has been prepared. Upon exposure to E. coli beta-glucuronidase, fast hydrolysis occurs but a lower cytotoxicity against LoVo cancer cells is observed compared to the nornitrogen mustard alone. This is explained by cyclization of the intermediate carbamic acid to the inactive chloroethyl oxazolidinone.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Papot S,Combaud D,Bosslet K,Gerken M,Czech J,Gesson JP

doi

10.1016/s0960-894x(00)00353-x

subject

Has Abstract

pub_date

2000-08-21 00:00:00

pages

1835-7

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(00)00353-X

journal_volume

10

pub_type

杂志文章

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