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Synthesis, in vitro screening and in vivo evaluation of cyclic RGD analogs cyclized through oxorhenium and oxotechnetium coordination.

Abstract：

:A library of RGD tripeptide analogs cyclized through oxorhenium coordination by an NS2/S chelation motif was synthesized. Screening towards integrins αVβ3, αIIbβ3 and αVβ5 led to the identification of 6 oxorhenium complexes that bind to integrin αVβ3 in the submicromolar range. In vivo evaluation of five of the corresponding oxotechnetium complexes using nude mice bearing a U87MG human tumor xenograft showed a significant and specific accumulation of radioactivity inside the tumor. The best results in vivo were obtained with complexes Tc-16 and Tc-50 that displayed a higher tumor accumulation and a lower distribution in other tissues relative to a reference cyclopentapeptide tracer.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Aufort M,Gonera M,Lelait MA,Czarny B,Le Clainche L,Thaï R,Landra A,Ruinart de Brimont M,Dugave C

doi

10.1016/j.ejmech.2011.02.032

subject

Has Abstract

pub_date

2011-05-01 00:00:00

pages

1779-88

issue

5

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00143-7

journal_volume

46

pub_type

杂志文章

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