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Technetium-99m-labeled hynic-containing palbociclib derivatives, preparation method and application

A technology of palbociclib and its derivatives, applied to the 7/17 group organic compounds without C-metal bonds, organic chemical methods, chemical instruments and methods, etc., can solve the problem of unsuitable tumor imaging agents and tumor imaging There are not many researches on the agent, poor stability and other problems

Active Publication Date: 2020-04-28
BEIJING NORMAL UNIVERSITY
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Problems solved by technology

[0005] At present, there are not many studies on radiolabeled CDK4 / 6 inhibitors as tumor imaging agents. In 2010, Koehler et al. reported two 124 I labeled compound ([ 124 I] CKIA and [ 124 I]CKIB, Eur.J.Med. Chem.2010,45,727–737), and explored its possibility as a tumor imaging agent, the experimental results showed that the stability of these two markers in rats was poor , so it is not suitable as a tumor imaging agent

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  • Technetium-99m-labeled hynic-containing palbociclib derivatives, preparation method and application
  • Technetium-99m-labeled hynic-containing palbociclib derivatives, preparation method and application
  • Technetium-99m-labeled hynic-containing palbociclib derivatives, preparation method and application

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Embodiment Construction

[0037] Describe the present invention in detail below by embodiment: a kind of 99m Tc-labeled palbociclib derivatives containing HYNIC, the general molecular formula is 99m Tc(HYNICPBB)(tricine / TPPTS), its structural formula is as follows:

[0038]

[0039] In the structural formula: the nitrogen atom on the hydrazine group in the HYNICPBB molecule, the phosphorus atom in the co-ligand TPPTS, and the oxygen and nitrogen atoms in the tricine and 99m Tc coordinates to get 99m Tc(HYNICPBB)(tricine / TPPTS).

[0040] 99m The specific preparation steps of Tc(HYNICPBB)(tricine / TPPTS) are as follows:

[0041] a. Synthesis of ligand HYNICPBB:

[0042] Weigh 447 mg of palbociclib and 440 mg of compound C into a 100 mL round bottom flask, add 200 μL of triethylamine and 30 mL of dichloromethane, and react at room temperature for 6 h. After the reaction, the solvent was removed by rotary evaporation, the crude product was separated and purified by silica gel column chromatography ...

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Abstract

The invention discloses a <99m>Tc(HYNICPBB)(tricine / TPPTS) complex as well as a preparation method and an application. The <99m>Tc(HYNICPBB)(tricine / TPPTS) complex is obtained through two steps including synthesis of a ligand HYNICPBB and preparation of <99m>Tc(HYNICPBB)(tricine / TPPTS). The complex is simple to prepare, high in radiochemical purity and good in stability, has better water solubility and has certain uptake in MCF-7 cells, the uptake can be significantly inhibited by palbociclib, which indicates that the complex has a CDK4 / 6 specificity. The complex has higher uptake and retention and better tumor / muscle ratios at tumor parts of female Balb / c nude mice carrying MCF-7 tumor, has obviously reduced uptake of non-target organs such as liver and can be applied to preparation of anovel CDK4 / 6 targeting tumor developer.

Description

technical field [0001] The present invention relates to 99m The field of Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology, specifically relates to a 99m Tc-labeled palbociclib derivative containing HYNIC, its preparation method and application. Background technique [0002] At present, malignant tumors have become the main killer of human health. The latest global cancer statistics report shows that in 2018, there were 18.1 million new cancer cases worldwide and 9.6 million people died of cancer. The 2015 China Cancer Statistics Report pointed out that 50% of Chinese cancer patients The annual survival rate is only 36.9%. This is because many patients have already undergone regional or distant metastasis when the disease is diagnosed. Therefore, early detection and treatment of cancer can improve the survival rate of patients and reduce the death of patients. It is of great significance to improve the rate, reduce the suffering of patients ...

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F13/00A61K51/04A61K103/10
CPCA61K51/0482C07B2200/05C07F13/005
Inventor 张俊波宋晓庆甘倩倩张旭冉王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
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