Journal of medicinal and pharmaceutical chemistry 2013-10-24

Gadolinium complex of DO3A-benzothiazole aniline (BTA) conjugate as a theranostic agent.

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 Kim

Index: J. Med. Chem. 56(20) , 8104-11, (2013)

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Abstract

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)(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.