Jung, Ki‐Hye;
Kang, Sun‐Hee;
Kang, Min‐Kyoung;
Kim, Soyeon;
Kim, Hee‐Kyung;
Kim, Yeoun‐Hee;
Ho Lee, Gang;
Shim, Gyu‐Bo;
Jung, Jae‐Chang;
Chang, Yongmin;
Kim, Tae‐Jeong
Synthesis and Structure–Activity Relationships of Gadolinium Complexes of DO3A–Benzothiazole Conjugates as Potential Theranostic Agents
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Medientyp:
E-Artikel
Titel:
Synthesis and Structure–Activity Relationships of Gadolinium Complexes of DO3A–Benzothiazole Conjugates as Potential Theranostic Agents
Beteiligte:
Jung, Ki‐Hye;
Kang, Sun‐Hee;
Kang, Min‐Kyoung;
Kim, Soyeon;
Kim, Hee‐Kyung;
Kim, Yeoun‐Hee;
Ho Lee, Gang;
Shim, Gyu‐Bo;
Jung, Jae‐Chang;
Chang, Yongmin;
Kim, Tae‐Jeong
Erschienen:
Wiley, 2015
Erschienen in:European Journal of Inorganic Chemistry
Beschreibung:
<jats:title>Abstract</jats:title><jats:p>The synthesis of two bifunctional chelates, 1,4,7,10‐tetraazacyclododecane‐1,4,7‐triacetic acid (DO3A) conjugates of benzothiazoles (H<jats:sub>3</jats:sub>L<jats:sup>3a</jats:sup> and H<jats:sub>3</jats:sub>L<jats:sup>3b</jats:sup>), and the corresponding gadolinium complexes (GdL<jats:sup>3a</jats:sup> and GdL<jats:sup>3b</jats:sup>) was achieved. The intracellular and tumor‐specific nature of GdL<jats:sup>3a</jats:sup> and GdL<jats:sup>3b</jats:sup> were confirmed by magnetic resonance images of the cytosols and nuclei of various cell lines. The two complexes displayed antitumor activities with varying degrees of growth‐inhibition and total‐growth‐inhibition values depending on the types of tumor cells. They caused morphological changes in tumor cell lines at much lower concentrations of gadolinium ([Gd] ≥ 50 μ<jats:sc>M</jats:sc>) than their predecessors, DO3A–(<jats:italic>p</jats:italic>‐aniline benzothiazole) conjugates (H<jats:sub>3</jats:sub>L<jats:sup>1</jats:sup>), and its Gd<jats:sup>III</jats:sup> complex (GdL<jats:sup>1</jats:sup>) required concentrations that were almost four times as high ([Gd] ≥ 200 μ<jats:sc>M</jats:sc>).</jats:p>