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Synthesis and Structure-Activity Relationships of Gadolinium Complexes of DO3A-Benzothiazole Conjugates as Potential Theranostic Agents.
- Source :
- European Journal of Inorganic Chemistry; Feb2015, Vol. 2015 Issue 4, p599-604, 6p
- Publication Year :
- 2015
-
Abstract
- The synthesis of two bifunctional chelates, 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid (DO3A) conjugates of benzothiazoles (H<subscript>3</subscript>L<superscript>3a</superscript> and H<subscript>3</subscript>L<superscript>3b</superscript>), and the corresponding gadolinium complexes (GdL<superscript>3a</superscript> and GdL<superscript>3b</superscript>) was achieved. The intracellular and tumor-specific nature of GdL<superscript>3a</superscript> and GdL<superscript>3b</superscript> 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 M) than their predecessors, DO3A-( p-aniline benzothiazole) conjugates (H<subscript>3</subscript>L<superscript>1</superscript>), and its Gd<superscript>III</superscript> complex (GdL<superscript>1</superscript>) required concentrations that were almost four times as high ([Gd] ≥ 200 μ M). [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 14341948
- Volume :
- 2015
- Issue :
- 4
- Database :
- Complementary Index
- Journal :
- European Journal of Inorganic Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 100748988
- Full Text :
- https://doi.org/10.1002/ejic.201403123