Phthalocyanine Labels for Near-Infrared Fluorescence Imaging of Solid Tumors

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• 作者：Ana C. S. Lobo ; Alexandre D. Silva ; Vanessa A. Tomé ; Sara M. A. Pinto ; Elsa F. F. Silva ; Mário J. F. Calvete ; Célia M. F. Gomes ; Mariette M. Pereira ; Luis G. Arnaut
• 刊名：Journal of Medicinal Chemistry
• 出版年：2016
• 出版时间：May 26, 2016
• 年：2016
• 卷：59
• 期：10
• 页码：4688-4696
• 全文大小：543K
• 年卷期：0
• ISSN：1520-4804

文摘

Diamagnetic metal complexes of phthalocyanines with n-butoxyl groups in all the α-benzo positions of the macrocycle skeleton, MPc(OBu)₈, have strong near-infrared absorptions and intense fluorescences that are Stokes shifted by more than 15 nm. Interestingly, the silicon complex 6 is also remarkably photostable and nontoxic. The use of 6 in the fluorescence imaging of BALB/c mice bearing a 4T1-luc2 tumor in the mammary fat pad unambiguously revealed the presence of the tumor when it was only 1 mm in diameter and was not visible with the naked eye. Compound 6 has an intrinsic ability to accumulate in the tumor, adequate spectroscopic properties, and excellent stability to function as a NIR fluorescent label in the early detection of tumors.