Novel Chlorin with a HYNIC: Synthesis, <sup>99m</sup>Tc-Radiolabeling, and Initial Preclinical Evaluation

The use of radiopharmaceuticals for diagnostics in oncology allows for the detection of the disease at an early stage. Among diagnostic radionuclides, <sup>99m</sup>Tc is a promising isotope that has been used to create several drugs for clinical use. One of the most effective <sup>...

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Main Authors: Alexander Popov, Nikita Suvorov, Mariia Larkina, Evgenii Plotnikov, Ruslan Varvashenya, Vitalina Bodenko, Gleb Yanovich, Petr Ostroverkhov, Maxim Usachev, Elena Filonenko, Mikhail Belousov, Mikhail Grin
Format: Article
Language:English
Published: MDPI AG 2024-12-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/1/117
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author Alexander Popov
Nikita Suvorov
Mariia Larkina
Evgenii Plotnikov
Ruslan Varvashenya
Vitalina Bodenko
Gleb Yanovich
Petr Ostroverkhov
Maxim Usachev
Elena Filonenko
Mikhail Belousov
Mikhail Grin
author_facet Alexander Popov
Nikita Suvorov
Mariia Larkina
Evgenii Plotnikov
Ruslan Varvashenya
Vitalina Bodenko
Gleb Yanovich
Petr Ostroverkhov
Maxim Usachev
Elena Filonenko
Mikhail Belousov
Mikhail Grin
author_sort Alexander Popov
collection DOAJ
description The use of radiopharmaceuticals for diagnostics in oncology allows for the detection of the disease at an early stage. Among diagnostic radionuclides, <sup>99m</sup>Tc is a promising isotope that has been used to create several drugs for clinical use. One of the most effective <sup>99m</sup>Tc chelators is 6-hydrazinylnicotinic acid (HYNIC), which, when combined with various vector molecules, can be used for targeted delivery of radionuclides to tumor tissues. At the same time, it is known that tetrapyrrole macrocycles are capable of selective accumulation in tumors, and thus can be used to target radiopharmaceuticals with <sup>99m</sup>Tc. In this work, the conjugate of natural chlorin and HYNIC was obtained, and preliminary preclinical studies were carried out on its radiocomplex with <sup>99m</sup>Tc.
format Article
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institution Kabale University
issn 1420-3049
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publishDate 2024-12-01
publisher MDPI AG
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series Molecules
spelling doaj-art-128ac9ee855b49a5a6138c0fad7af1e62025-01-10T13:18:56ZengMDPI AGMolecules1420-30492024-12-0130111710.3390/molecules30010117Novel Chlorin with a HYNIC: Synthesis, <sup>99m</sup>Tc-Radiolabeling, and Initial Preclinical EvaluationAlexander Popov0Nikita Suvorov1Mariia Larkina2Evgenii Plotnikov3Ruslan Varvashenya4Vitalina Bodenko5Gleb Yanovich6Petr Ostroverkhov7Maxim Usachev8Elena Filonenko9Mikhail Belousov10Mikhail Grin11M. V. Lomonosov Institute of Fine Chemical Technology, MIREA—Russian Technological University, 86 Vernadsky Av., 119571 Moscow, RussiaM. V. Lomonosov Institute of Fine Chemical Technology, MIREA—Russian Technological University, 86 Vernadsky Av., 119571 Moscow, RussiaScience and Education Laboratory for Chemical and Pharmaceutical Research, Siberian State Medical University, 634050 Tomsk, RussiaScience and Education Laboratory for Chemical and Pharmaceutical Research, Siberian State Medical University, 634050 Tomsk, RussiaScience and Education Laboratory for Chemical and Pharmaceutical Research, Siberian State Medical University, 634050 Tomsk, RussiaScience and Education Laboratory for Chemical and Pharmaceutical Research, Siberian State Medical University, 634050 Tomsk, RussiaScience and Education Laboratory for Chemical and Pharmaceutical Research, Siberian State Medical University, 634050 Tomsk, RussiaM. V. Lomonosov Institute of Fine Chemical Technology, MIREA—Russian Technological University, 86 Vernadsky Av., 119571 Moscow, RussiaM. V. Lomonosov Institute of Fine Chemical Technology, MIREA—Russian Technological University, 86 Vernadsky Av., 119571 Moscow, RussiaM. V. Lomonosov Institute of Fine Chemical Technology, MIREA—Russian Technological University, 86 Vernadsky Av., 119571 Moscow, RussiaDepartment of Pharmaceutical Analysis, Siberian State Medical University, 634050 Tomsk, RussiaM. V. Lomonosov Institute of Fine Chemical Technology, MIREA—Russian Technological University, 86 Vernadsky Av., 119571 Moscow, RussiaThe use of radiopharmaceuticals for diagnostics in oncology allows for the detection of the disease at an early stage. Among diagnostic radionuclides, <sup>99m</sup>Tc is a promising isotope that has been used to create several drugs for clinical use. One of the most effective <sup>99m</sup>Tc chelators is 6-hydrazinylnicotinic acid (HYNIC), which, when combined with various vector molecules, can be used for targeted delivery of radionuclides to tumor tissues. At the same time, it is known that tetrapyrrole macrocycles are capable of selective accumulation in tumors, and thus can be used to target radiopharmaceuticals with <sup>99m</sup>Tc. In this work, the conjugate of natural chlorin and HYNIC was obtained, and preliminary preclinical studies were carried out on its radiocomplex with <sup>99m</sup>Tc.https://www.mdpi.com/1420-3049/30/1/117technetium-99mchlorinradiopharmaceuticalsHYNICcancer
spellingShingle Alexander Popov
Nikita Suvorov
Mariia Larkina
Evgenii Plotnikov
Ruslan Varvashenya
Vitalina Bodenko
Gleb Yanovich
Petr Ostroverkhov
Maxim Usachev
Elena Filonenko
Mikhail Belousov
Mikhail Grin
Novel Chlorin with a HYNIC: Synthesis, <sup>99m</sup>Tc-Radiolabeling, and Initial Preclinical Evaluation
Molecules
technetium-99m
chlorin
radiopharmaceuticals
HYNIC
cancer
title Novel Chlorin with a HYNIC: Synthesis, <sup>99m</sup>Tc-Radiolabeling, and Initial Preclinical Evaluation
title_full Novel Chlorin with a HYNIC: Synthesis, <sup>99m</sup>Tc-Radiolabeling, and Initial Preclinical Evaluation
title_fullStr Novel Chlorin with a HYNIC: Synthesis, <sup>99m</sup>Tc-Radiolabeling, and Initial Preclinical Evaluation
title_full_unstemmed Novel Chlorin with a HYNIC: Synthesis, <sup>99m</sup>Tc-Radiolabeling, and Initial Preclinical Evaluation
title_short Novel Chlorin with a HYNIC: Synthesis, <sup>99m</sup>Tc-Radiolabeling, and Initial Preclinical Evaluation
title_sort novel chlorin with a hynic synthesis sup 99m sup tc radiolabeling and initial preclinical evaluation
topic technetium-99m
chlorin
radiopharmaceuticals
HYNIC
cancer
url https://www.mdpi.com/1420-3049/30/1/117
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