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99mTc labeled macrocyclic aza-oxa and aza-thia probes: synthesis, characterization and in vitro & in vivo biological studies

  • Neelam Yadav
  • Krishna Chuttani
  • Anil K. Mishra
  • Bachcha Singh
Original Article
  • 140 Downloads

Abstract

Macrocyclic chelating agents 1-oxa-4,7,10-triazacyclopentadecane-3,11-dione (OTDD) and 1-thia-4,7, 10-triazacyclododecane-3,11-dione (TTDD) have been synthesized and labeled with radionuclide (99mTc), with radiolabeling efficiency 97.6 and 98.4 % respectively. The radiochemical purity of labeled complex (99mTc-OTDD and 99mTc-TTDD) was determined 97.5 and 98.1 %, respectively. The in vitro stability of the labeled chelates in human serum exhibited only <8 % dissociation upto 24 h. The in vivo distribution pattern of the labeled chelators in BALB/c mice suggested that major route of excretion in 99mTc-TTDD is hepatobilliary and minor is renal, while in case of 99mTc-OTDD hepatobilliary as well as renal both comparable. The in vivo blood kinetic studies of radio-complexes of 99mTc-OTDD and 99mTc-TTDD showed 99.26 and 99.4 % blood clearance over 24 h post injection. The biological half-life of 99mTc-OTDD and 99mTc-TTDD with t1/2(F) 1 h 10 min, t1/2(S) 18 h 50 min and t1/2(F) 1 h 42 min, t1/2(S) 18 h 20 min respectively. In vitro cytotoxicity study of OTDD and TTDD did not exhibit any significant antiproliferative property against cancer cells of human glioblastoma U-87, U373 and cervical SW756, HeLa cell lines.

Keywords

Cancer Macrocyclic chelating agents 99mTc DFT Radiolabeling 

Notes

Acknowledgments

We are grateful to the Head, Department of Chemistry (Center of Advanced Study), Faculty of Science, Banaras Hindu University, Varanasi, for extending laboratory facilities. N.Y. gratefully acknowledges UGC, New Delhi for awarding JRF UGC-BSR fellowship.

Compliance with ethical standards

Conflict of interest

The authors declare no conflict of interest.

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Copyright information

© Springer Science+Business Media Dordrecht 2015

Authors and Affiliations

  • Neelam Yadav
    • 1
  • Krishna Chuttani
    • 2
  • Anil K. Mishra
    • 2
  • Bachcha Singh
    • 1
  1. 1.Department of Chemistry (Centre of Advanced Study), Faculty of ScienceBanaras Hindu UniversityVaranasiIndia
  2. 2.Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied SciencesDefence Research and Development OrganizationDelhiIndia

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