Gadolinium complex of DO3A-benzothiazole aniline (BTA) conjugate as a theranostic agent.
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.
Department of Medical & Biological Engineering, ‡Department of Applied Chemistry, §Department of Biology, ∥Department of Chemistry, ⊥Department of Diagnostic Radiology and Molecular Medicine, Kyungpook National University , 80 Daehakro, Bukgu, Daegu, 702-701, Korea.
Hee-Kyung
HK
Kim
Min-Kyoung
MK
Kang
Ki-Hye
KH
Jung
Sun-Hee
SH
Kang
Yeoun-Hee
YH
Kim
Jae-Chang
JC
Jung
Gang Ho
GH
Lee
Yongmin
Y
Chang
Tae-Jeong
TJ
Kim
D000818:Animals; D052160:Benzothiazoles / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D003287:Contrast Media / Q000737:chemistry; D005260:Female; D005682:Gadolinium / Q000737:chemistry*; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D006801:Humans; D061986:MCF-7 Cells; D008279:Magnetic Resonance Imaging / Q000379:methods; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D015394:Molecular Structure; D009369:Neoplasms / Q000175:diagnosis / Q000188:drug therapy / Q000473:pathology; D009942:Organometallic Compounds / Q000737:chemistry* / Q000494:pharmacology; D012680:Sensitivity and Specificity; D023041:Xenograft Model Antitumor Assays
C520644:1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid; D052160:Benzothiazoles; D003287:Contrast Media; D006573:Heterocyclic Compounds, 1-Ring; D009942:Organometallic Compounds; D005682:Gadolinium; C005465:benzothiazole