Startseite Synthesis and radiolabelling studies of hynic conjugated PSMA targeting ligands
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Synthesis and radiolabelling studies of hynic conjugated PSMA targeting ligands

  • K. S. Ajish Kumar ORCID logo EMAIL logo und Madhava B. Mallia ORCID logo
Veröffentlicht/Copyright: 16. Juni 2025
Radiochimica Acta
Aus der Zeitschrift Radiochimica Acta Band 113 Heft 8

Abstract

Development and clinical translation of small molecule PSMA-ligands labelled with a SPECT-radioisotope such as technetium-99m (99mTc) has immense importance, particularly in countries with high population density and limited amenities. Towards this, herein we report the total chemical synthesis of five Hynic (2-hydrazinonicotinic acid) conjugated PSMA ligands employing the solution phase alloc chemistry. A linear synthetic strategy was adopted for the construction of all target molecules. The amino acids that act as spacers were synthesized from corresponding unprotected precursors in 60–65 % overall yield. All the synthesized ligands were appropriately characterized using NMR, HPLC, and MS, to confirm their structural veracity. After the successful synthesis, all the ligands were radiolabelled using 99mTc and the extent of 99mTc radiolabelling was established using radioHPLC and radioTLC analysis. Two among the five ligands displayed radiochemical purity >90 %, adequate for diagnostic applications.

Keywords: ligand; diagnosis; hynic; radionuclide; prostate
Corresponding author: K. S. Ajish Kumar, Bio-Organic Division, Bhabha Atomic Research Centre, Mumbai, India; and Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India, E-mail:

Acknowledgments

KSAK thankfully acknowledge Prof. B. S Patro, Head, Bio-Organic Division, Prof. P. A. Hassan, Associate Group Director, Bio Science Group for their constant support and encouragement throughout the course of this activity. We are grateful to the support from National NMR Facility, TIFR, Mumbai. KSAK is highly thankful to Dr. Anupam Mathur, BRIT, Vashi for his enthusiasm and support.

  1. Research ethics: Not applicable.

  2. Informed consent: Not applicable.

  3. Author contributions: All authors have accepted responsibility for the entire content of this manuscript and approved its submission.

  4. Use of Large Language Models, AI and Machine Learning Tools: None declared.

  5. Conflict of interest: The authors state no conflict of interest.

  6. Research funding: None declared.

  7. Data availability: The data can be obtained on request from the corresponding author.

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Received: 2025-03-18
Accepted: 2025-05-30
Published Online: 2025-06-16
Published in Print: 2025-08-26

© 2025 Walter de Gruyter GmbH, Berlin/Boston

Artikel in diesem Heft

  1. Frontmatter
  2. Original Papers
  3. First principles modeling of plutonium complexation in nitric and hydrochloric acid solutions
  4. Positron emission intensity in the decay of 72As for use in PET studies
  5. The application of nuclear technique for measuring the bioaccumulation of microplastic in oyster (Crassostera Gigas)
  6. Synthesis and radiolabelling studies of hynic conjugated PSMA targeting ligands
  7. Impact of gamma and electron-beam irradiations on the thermal dehydration process of europium acetate hydrate
  8. Synthesis, mechanical, and radiation-attenuation characteristics of aluminium phosphate glass system modified by NiO/Li2O
  9. Preparation, physical, structural, and radiation shielding characteristics of SiO2–TiO2–B2O3–ZrO2 glass ceramics
https://doi.org/10.1515/ract-2025-0038
Schlagwörter für diesen Artikel
ligand; diagnosis; hynic; radionuclide; prostate

Artikel in diesem Heft

  1. Frontmatter
  2. Original Papers
  3. First principles modeling of plutonium complexation in nitric and hydrochloric acid solutions
  4. Positron emission intensity in the decay of 72As for use in PET studies
  5. The application of nuclear technique for measuring the bioaccumulation of microplastic in oyster (Crassostera Gigas)
  6. Synthesis and radiolabelling studies of hynic conjugated PSMA targeting ligands
  7. Impact of gamma and electron-beam irradiations on the thermal dehydration process of europium acetate hydrate
  8. Synthesis, mechanical, and radiation-attenuation characteristics of aluminium phosphate glass system modified by NiO/Li2O
  9. Preparation, physical, structural, and radiation shielding characteristics of SiO2–TiO2–B2O3–ZrO2 glass ceramics
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