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一种含HYNIC的新型二氢卟吩:合成、锝放射性标记及初步临床前评估。

Novel Chlorin with a HYNIC: Synthesis, Tc-Radiolabeling, and Initial Preclinical Evaluation.

作者信息

Popov Alexander, Suvorov Nikita, Larkina Mariia, Plotnikov Evgenii, Varvashenya Ruslan, Bodenko Vitalina, Yanovich Gleb, Ostroverkhov Petr, Usachev Maxim, Filonenko Elena, Belousov Mikhail, Grin Mikhail

机构信息

M. V. Lomonosov Institute of Fine Chemical Technology, MIREA-Russian Technological University, 86 Vernadsky Av., 119571 Moscow, Russia.

Science and Education Laboratory for Chemical and Pharmaceutical Research, Siberian State Medical University, 634050 Tomsk, Russia.

出版信息

Molecules. 2024 Dec 31;30(1):117. doi: 10.3390/molecules30010117.

Abstract

The use of radiopharmaceuticals for diagnostics in oncology allows for the detection of the disease at an early stage. Among diagnostic radionuclides, Tc is a promising isotope that has been used to create several drugs for clinical use. One of the most effective 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 Tc. In this work, the conjugate of natural chlorin and HYNIC was obtained, and preliminary preclinical studies were carried out on its radiocomplex with Tc.

摘要

放射性药物在肿瘤学诊断中的应用能够在疾病早期实现检测。在诊断用放射性核素中,锝是一种很有前景的同位素,已被用于研发多种临床用药。最有效的锝螯合剂之一是6-肼基烟酸(HYNIC),它与各种载体分子结合后,可用于将放射性核素靶向递送至肿瘤组织。同时,已知四吡咯大环能够在肿瘤中选择性蓄积,因此可用于靶向含锝的放射性药物。在这项工作中,制备了天然二氢卟吩与HYNIC的缀合物,并对其与锝的放射性配合物进行了初步临床前研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef56/11721277/b556e8ef62a0/molecules-30-00117-sch001.jpg

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