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Design, characterization and evaluation of a new Tc-labeled folate derivative with affinity towards folate receptor.

Bioorg Med Chem Lett

April 2023

Homi Bhabha National Institute (HBNI), Anushaktinagar, Mumbai 400094, India; Radiopharmaceutical Division, Bhabha Atomic Rweesearch Centre (BARC), Trombay, Mumbai 400085, India. Electronic address:

Folate receptors (FRs) are known to be over-expressed in several human malignancies and therefore serve as an important target for small radiolabeled folate derivatives for non-invasive imaging of tumor, which is an important tool for future treatment recourse. In the present article, we report the synthesis of a new Tc-labeled radiotracer for the aforementioned application following the well-established Tc-'4+1' chemistry. Formation of the desired [Tc]Tc-complex with >95% radiochemical purity was confirmed by radio-HPLC and its structure was ascertained by characterizing a natural rhenium analogue of the said complex.

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