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Gadolinium complex of DO3A-benzothiazole aniline (BTA) conjugate as a theranostic agent.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2013 Oct 24; Vol. 56 (20), pp. 8104-11. Date of Electronic Publication: 2013 Oct 10. - Publication Year :
- 2013
-
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.
- Subjects :
- Animals
Cell Line, Tumor
Cell Proliferation drug effects
Cell Survival drug effects
Contrast Media chemistry
Female
Humans
MCF-7 Cells
Magnetic Resonance Imaging methods
Mice
Mice, Inbred BALB C
Mice, Nude
Molecular Structure
Neoplasms diagnosis
Neoplasms drug therapy
Neoplasms pathology
Organometallic Compounds pharmacology
Sensitivity and Specificity
Xenograft Model Antitumor Assays
Benzothiazoles chemistry
Gadolinium chemistry
Heterocyclic Compounds, 1-Ring chemistry
Organometallic Compounds chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 56
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 24063520
- Full Text :
- https://doi.org/10.1021/jm401206t