Gadolinium Complex of DO3A-benzothiazole Aniline (BTA) Conjugate as a Theranostic Agent

다국어 초록 (Multilingual Abstract)

<P>A gadolinium complex of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid (DO3A) and benzothiazole-aniline (BTA) of the type [Gd(DO3A-BTA)(H<SUB>2</SUB>O)] has been prepared for use as a single molecule theranostic agent. The kinetic inertness and <I>r</I><SUB>1</SUB> relaxivity (= 3.84 mM<SUP>–1</SUP> s<SUP>–1</SUP>) of the complex compare well with those of structurally analogous Gd-DOTA. The same complex is not only tumor-specific but also intracellular, enhancing MR images of cytosols and nuclei of tumor cells such as MCF-7, MDA-MB-231, and SK-HEP-1. Both DO3A-BTA and Gd(DO3A-BTA) reveal antiproliferative activities as demonstrated by GI<SUB>50</SUB> and TGI values obtainable from the cell counting kit-8 (CCK-8) assays performed on these cell lines. Ex vivo and in vivo monitoring of tumor sizes provide parallel and supportive observations for such antiproliferative activities.</P><P><B>Graphic Abstract</B>
<IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jmcmar/2013/jmcmar.2013.56.issue-20/jm401206t/production/images/medium/jm-2013-01206t_0006.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/jm401206t'>ACS Electronic Supporting Info</A></P>