10.1021/jm401206t.s001
Hee-Kyung Kim
Hee-Kyung
Kim
Min-Kyoung Kang
Min-Kyoung
Kang
Ki-Hye Jung
Ki-Hye
Jung
Sun-Hee Kang
Sun-Hee
Kang
Yeoun-Hee Kim
Yeoun-Hee
Kim
Jae-Chang Jung
Jae-Chang
Jung
Gang Ho Lee
Gang Ho
Lee
Yongmin Chang
Yongmin
Chang
Tae-Jeong Kim
Tae-Jeong
Kim
Gadolinium Complex of DO3A-benzothiazole
Aniline (BTA)
Conjugate as a Theranostic Agent
American Chemical Society
2013
CCK
Theranostic AgentA gadolinium
3A
vivo
TGI
MR
GI
MCF
tumor
Gd
BTA
molecule theranostic agent
antiproliferative activities
2013-10-24 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Gadolinium_Complex_of_DO3A_benzothiazole_Aniline_BTA_Conjugate_as_a_Theranostic_Agent/2362843
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.