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Technetium-99m labeled palbociclib derivative containing HYNIC as well as preparation method and application

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

Active Publication Date: 2019-08-02
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 palbociclib derivative containing HYNIC as well as preparation method and application
  • Technetium-99m labeled palbociclib derivative containing HYNIC as well as preparation method and application
  • Technetium-99m labeled palbociclib derivative containing HYNIC as well as preparation method and application

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[0038] The present invention is described in detail below by examples: a 99m Tc-labeled HYNIC-containing Palbociclib derivatives, the general formula is 99m Tc(HYNICPBB)(tricine / TPPTS), its structural formula is as follows:

[0039]

[0040] In this 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 tricine are related to 99m Tc coordinate to get 99m Tc(HYNICPBB)(tricine / TPPTS).

[0041] 99m The specific preparation steps of Tc(HYNICPBB)(tricine / TPPTS) are as follows:

[0042] a. Synthesis of ligand HYNICPBB:

[0043] 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, and the crude product was separated and purified by silica gel column chromatography (dich...

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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 Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology fields, specifically involving a 99m Tc-labeled HYNIC-containing Palbociclib derivatives, preparation method and application. Background technique [0002] At present, malignant tumors have become the main killers that endanger human health. The latest global cancer statistics report shows that in 2018, there were 18.1 million new cancer cases and 9.6 million deaths due to cancer in the world. The 2015 China Cancer Statistics Report pointed out that five 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 early treatment of cancer can improve the survival rate and reduce the death of patients. It is of great significance to improve the efficiency, reduce the suffering of patients and save the cost of t...

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Application Information

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Patent Type & Authority Applications(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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