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Isosteres of ester derived glucose uptake inhibitors.

Abstract：

:Glucose transporters (GLUTs) facilitate glucose uptake and are overexpressed in most cancer cells. Inhibition of glucose transport has been shown to be an effective method to slow the growth of cancer cells both in vitro and in vivo. We have previously reported on the anticancer activity of an ester derived glucose uptake inhibitor. Due to the hydrolytic instability of the ester linkage we have prepared a series of isosteres of the ester moiety. Of all of the isosteres prepared, the amine linkage showed the most promise. Several additional analogues of the amine-linked compounds were also prepared to improve the overall activity.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Roberts DA,Wang L,Zhang W,Liu Y,Shriwas P,Qian Y,Chen X,Bergmeier SC

doi

10.1016/j.bmcl.2020.127406

subject

Has Abstract

pub_date

2020-09-15 00:00:00

pages

127406

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(20)30517-5

journal_volume

30

pub_type

杂志文章

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