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

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• 作者：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
• 刊名：Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：October 24, 2013
• 年：2013
• 卷：56
• 期：20
• 页码：8104-8111
• 全文大小：427K
• 年卷期：v.56,no.20(October 24, 2013)
• ISSN：1520-4804

文摘

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^鈥? s^鈥?) 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.