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Small-molecule inhibitor SLD1338 and application thereof in pharmacy

A technology of small molecule inhibitors and drugs, applied in drug combinations, antineoplastic drugs, organic chemistry, etc., can solve the problems of insignificant effect, little effect, and low toxicity effect in advanced breast cancer

Active Publication Date: 2018-04-06
CHINA THREE GORGES UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the phase II clinical study, it was found that BENSpm as a single drug has no significant effect on the treatment of advanced breast cancer, and the extended experiment for this study shows that BENSpm has a synergistic effect when used in combination with other conventional chemotherapy drugs
The second-generation spermine analog CPENSpm has lower toxicity and more significant effect than the first generation, but CPENSpm and BENSpm face the same problem and must be used in combination with other chemotherapy drugs
Although BENSpm and CPENSpm have good prospects for clinical application from the results of preclinical experiments, they have had little effect in phase I and II clinical trials

Method used

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  • Small-molecule inhibitor SLD1338 and application thereof in pharmacy
  • Small-molecule inhibitor SLD1338 and application thereof in pharmacy
  • Small-molecule inhibitor SLD1338 and application thereof in pharmacy

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0036] A small molecule inhibitor SLD1338, characterized in that the structural formula of the small molecule inhibitor is:

[0037]

[0038] Pharmacophore results

[0039] In the complex structure, a lot of hydrogen bond interactions are formed between Spd and SMO. In order to ensure the rationality of the pharmacophore model, we only kept two pairs of key hydrogen bond characteristic elements. In addition, in order to ensure the diversity of the structure, after analyzing the characteristics of the active pocket, we added a set of hydrogen bond characteristic elements based on acceptor amino acids P1-Ser O. details as follows( figure 1 ): two donor centers - P1-Ser O and P3-Glu O.

[0040] Molecular docking results

[0041] The compounds obtained through the above pharmacophore model search are optimized, and the optimized compounds are used in the next step of molecular docking screening, and are sorted according to the docking energy scoring. The selected 120 compo...

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Abstract

The invention provides a small-molecule inhibitor SLD1338. The structural formula of the small-molecule inhibitor is as shown in the description. The small-molecule inhibitor SLD1338 is applied to preparing a drug for inhibiting spermine oxidase. The result shows that the SLD1338 changes the growth cycle of human small cell lung cancer A549 cells and changes the expression content of A549 cyclin,and meanwhile can induce apoptosis of the A549 cells.

Description

technical field [0001] The invention provides a small-molecule inhibitor for inhibiting spermine oxidase, and the application of the small-molecule inhibitor in the preparation of drugs for treating tumor diseases. Background technique [0002] Polyamines (putrescine, spermidine, and spermine) are small molecular organic compounds widely present in eukaryotic cells, and participate in important physiological functions such as cell differentiation, proliferation, and gene regulation. Studies have found that high intracellular polyamine content is necessary for the rapid growth of tumor cells, so the polyamine metabolic pathway has gradually become a new target for anti-tumor therapy and drug design. Spermine oxidase (Spermine oxidase, SMO) is a key enzyme involved in the degradation and metabolism of polyamines. This enzyme is a FAD (flavin adenine dinucleotide)-dependent oxidase. Spm) oxidation as its preferred substrate decomposition pathway. The products of this enzyme a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/088A61P35/00
CPCC07D295/088
Inventor 曹春雨王艳林杨建林孙丽丹
Owner CHINA THREE GORGES UNIV
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