Development of hypoxia-sensitive Gd 3+-based MRI contrast agents

S Iwaki, K Hanaoka, W Piao, T Komatsu, T Ueno…

Index: Iwaki, Shimpei; Hanaoka, Kenjiro; Piao, Wen; Komatsu, Toru; Ueno, Tasuku; Terai, Takuya; Nagano, Tetsuo Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 8 p. 2798 - 2802

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Citation Number: 28

Abstract

Hypoxia occurs in various diseases, including cancer, ischemia, and acute and chronic vascular diseases. Here we describe the design and synthesis of the first hypoxia-sensitive MRI contrast agents, SAGds. SAGds showed a pH-dependent r1 relaxivity change associated with intramolecular chelation of the nitrogen atom of the sulfonamide moiety to the Gd3+ center. There was a correlation between the pKa of the r1 relaxivity change and ...