Preparation method of small-molecule inhibitor for prostate-specific membrane antigen

A small molecule inhibitor, prostate-specific technology, applied in the field of medicine

Active Publication Date: 2019-02-26
FUDAN UNIV SHANGHAI CANCER CENT
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] The purpose of the present invention is to provide a method for preparing a small molecule inhibitor of prostate specific membrane antigen, to solve the problem of using the small molecule targeting PSMA in the prior art as the core structure Lys-Urea-Glu preparation method of the inhibitor. lack of

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  • Preparation method of small-molecule inhibitor for prostate-specific membrane antigen
  • Preparation method of small-molecule inhibitor for prostate-specific membrane antigen
  • Preparation method of small-molecule inhibitor for prostate-specific membrane antigen

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Embodiment Construction

[0038] The preparation method of the small-molecule inhibitor of prostate-specific membrane antigen proposed by the present invention will be further described in detail below with reference to the accompanying drawings and specific examples. Advantages and features of the present invention will be apparent from the following description and claims. It should be noted that all the drawings are in a very simplified form and use imprecise scales, and are only used to facilitate and clearly assist the purpose of illustrating the embodiments of the present invention.

[0039] Embodiments of the present invention are described below through specific examples, and those skilled in the art can easily understand other advantages and effects of the present invention from the content disclosed in this specification. The present invention can also be implemented or applied through other different specific implementation modes, and various modifications or changes can be made to the detai...

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Abstract

The invention provides a preparation method of a small-molecule inhibitor for a prostate-specific membrane antigen. The preparation method comprises the following steps: taking a glutamic acid derivative and a lysine derivative as starting raw materials, and preparing a formula (IV) core structure Lys-Urea-Glu for a formula (I) small-molecule inhibitor by using a carbonyldiimidazole one-pot method; and removing a protecting group after the formula (IV) core structure Lys-Urea-Glu is connected with HYNIC with 99mTc chelating power through a connecting chain so as to obtain the formula (I) small-molecule inhibitor. If the small-molecule inhibitor (namely the formula (I) small-molecule inhibitor) for the prostate-specific membrane antigen prepared on the basis of the parathion method is marked by radioactive nuclide 99mTc, the small-molecule inhibitor can be used for the diagnosis of prostatic cancer clinically as a molecular imaging probe and has potential clinical application values.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a preparation method of a small molecule inhibitor of prostate specific membrane antigen. Background technique [0002] Prostate cancer is one of the most common tumors threatening men's health. In recent years, its incidence in my country has increased significantly, and it has become the fastest growing disease among all malignant tumors, and large cities have become "hardest hit areas". Prostate-specific membrane antigen (PSMA) is overexpressed on the surface of almost all prostate cancer cells, and its expression is further increased in poorly differentiated, metastatic and androgen-independent prostate cancer cells. Therefore, PSMA is important for the diagnosis and treatment of prostate cancer is a very attractive target. [0003] Literature (Nucl. Med. Biol., 2017, 48, 69-75) reported a compound targeting PSMA and its preparation method. Through solid-phase synthesis, ...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/82
CPCC07D213/82Y02P20/55
Inventor 吴平许晓平章英剑
Owner FUDAN UNIV SHANGHAI CANCER CENT
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