Preparation and preliminary biological evaluation of 99mTc-ANMdU

RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE

Preparation and preliminary biological evaluation of ^99mTc-ANMdU

LU Chunxiong ，

JIANG Quanfu，

YU Huixin，

WANG Songpei，

Li Xiaomin，

WANG Zhengwu

Nuclear Science and Techniques

Vol.21, No.2

pp.106-109

Published in print 20 Apr 2010

DOI：10.13538/j.1001-8042/nst.21.106-109

33100

Technetium-99m-labeled-5-{2-sulfanylethyl-[2-(2-sulfanylethylamino)acetyl]amino}-methyl-2′-deoxy- uridine (^99mTc-ANMdU) was reported. The precursor ANMdU was synthesized by six-step reactions and all intermediates were verified with MS and ¹HNMR. Using SnCl₂ as reducing agent, a labeling reaction was carried out at 100°C for 30 min. The radiochemical purity of the ^99mTc-ANMdU was 96.68%. Partition coefficients were 0.92 and 0.70 at pH 7.0 and 7.4 of the phosphate buffer saline, respectively. Biodistribution of ^99mTc-ANMdU in normal mice showed that the initial uptake of ^99mTc-ANMdU in vivo and the clearance was rapid.

Synthesis99mTc-ANMdUBiodistributionA thymidine analog

References

[1]

Shields A F, Grierson J R, Dohmen B M, et al. Nat Med, 1998, 4(11): 1334-1336.

[2]

Kubota R, Yamada S, Kubota K, et al. J Nucl Med, 1992, 33(11): 1972-1980.

[3]

Lu L, Samuelsson L, Bergstrfm M, et al. J Nucl Med, 2002, 43(12): 1688-1698.

[4]

Shields A F, J Nucl Med, 2003, 44(9): 1432-1434.

[5]

Barthel H, Perumal M, Latigo J, et al. Eur J Nucl Med Mol Imaging, 2005, 32(3): 257-263.

[6]

Barthel H, Cleij M C, Collingridge, D R, et al. Cancer Res, 2003, 63(13): 3791-3798.

[7]

Chen W, Cloughesy T, Kamdar N, et al. J Nucl Med, 2005, 46(6): 945-952.

[8]

Sun H, Sloan A, Mangner T J, et al. Eur J Nucl Med Mol Imaging, 2005, 32(1): 15-22.

[9]

Zhang Y, Dai X, Kallmes D F, et al. Tetrahedron Lett, 2004, 45(47): 8673-8676.

[10]

Teng B, Bai Y, Chang Y, et al. Bioorgan Med Chem Lett, 2007, 17(12): 3440-3444.

[11]

Celen S, Groot T, Balzarini J, et al. Nucl Med Bio, 2007, 34(3): 283-291.

[12]

Lu C, Wang Z, Jiang Q, et al. J Isoto, 2008, 21(3): 145-149. (in Chinese)