Quinazoline derivatives, composition and application thereof

A technology of quinazoline and derivatives, which is used in the preparation of anti-tumor drugs and in the field of treating malignant tumors, can solve the problems of lack of effective inhibition of PGK1, no reports on cell level and in vivo studies, and few reports on inhibitor studies.

Active Publication Date: 2018-03-20
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

PGK1 is a target closely related to tumor cell growth, but there are few reports on its inhibitors
In 2012, Abbott reported that a class of quinoxaline derivatives had PGK1 inhibitory activity, but the activity was only tested at the enzyme level, and there was no report on its further cell level and in vivo studies (WO 2012045196A1)
[0005] So far, there is still a lack of drugs that effectively inhibit PGK1 clinically

Method used

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  • Quinazoline derivatives, composition and application thereof
  • Quinazoline derivatives, composition and application thereof
  • Quinazoline derivatives, composition and application thereof

Examples

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Embodiment Construction

[0082] The present invention will be further described below in conjunction with specific examples, but these examples do not limit the scope of the present invention.

[0083] For the following examples, standard manipulations and purification methods known to those skilled in the art can be used. Unless otherwise specified, starting materials are generally available from commercial sources such as Aldrich Chemicals Co. and Acros Organics. Commercially available solvents and reagents were generally used without further purification, anhydrous solvents were processed by standard methods, and other reagents were commercially available analytically pure. Unless otherwise stated, all temperatures are expressed in °C (degrees Celsius), and room or ambient temperature refers to 20-25 °C. The structures of the compounds were determined by nuclear magnetic resonance spectroscopy (NMR). Proton NMR shifts (δ) are given in parts per million (ppm). The proton nuclear magnetic resonanc...

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Abstract

The invention relates to quinazoline derivatives as shown in a formula I as described in the specification, a composition and application thereof as a PGK1 inhibitor for preparing anti-tumor drugs andapplication thereof in treating malignant tumors.

Description

technical field [0001] The present invention relates to a class of quinazoline derivatives, their compositions and uses, specifically, the present invention relates to a class of quinazoline derivatives, their compositions and their use as PGK1 inhibitors in the preparation of antitumor drugs and in Use in the treatment of malignant tumors. Background technique [0002] Compared with normal cells, a prominent feature of tumor cells is the abnormal energy metabolism of tumor cells. Fast-growing tumor cells exhibit a higher rate of glycolysis than normal cells. Abnormal aerobic glycolysis not only provides a large amount of energy for the growth of tumor cells, but also produces nucleotides, fatty acids and amino acids necessary for tumor cell growth (Moreno-Sánchez R., Rodríguez-Enríquez S., Marín-Hernández A ., Saavedra E. Energy metabolism in tumor cells. FEBS J. 2007, 274, 1393-1418). There is increasing evidence (Koppenol W.H., Bounds P.L., Dang C.V. Otto Warburg's con...

Claims

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Application Information

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IPC IPC(8): C07D405/14C07D409/14C07D417/14C07D401/14C07D471/10A61K31/517A61K31/5377A61P35/00
CPCC07D401/14C07D405/14C07D409/14C07D417/14C07D471/10
Inventor张翱高大明倪嘉斌胡弘历丁春勇
OwnerSHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI