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Gadolinium Complex of DO3A-benzothiazole Aniline (BTA) Conjugate as a Theranostic Agent
journal contribution
posted on 2013-10-24, 00:00 authored by Hee-Kyung Kim, Min-Kyoung Kang, Ki-Hye Jung, Sun-Hee Kang, Yeoun-Hee Kim, Jae-Chang Jung, Gang Ho Lee, Yongmin Chang, Tae-Jeong KimA gadolinium complex of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic
acid (DO3A) and benzothiazole-aniline (BTA) of the type [Gd(DO3A-BTA)(H2O)] has been prepared for use as a single molecule theranostic
agent. The kinetic inertness and r1 relaxivity
(= 3.84 mM–1 s–1) 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 GI50 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.