Marine Biomedical Research Institute of Qingdao Co., Ltd.

Shenzhen Huahong Marine Biomedicine Co., Ltd.

Shenzhen Bgi Marine Sci & Tech Co., Ltd

Shixiao Wang

Huashi Guan

Wenbao Li

Zhongpeng Ding

Yingwei Hou

Feng Wang

Feng Li

Liang Zhang

Chong Yang

Tianwen Sun

Jianchun Zhao

Zhiyu Song

Bing Cai

Xianjun Qu

A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.

Polycrystalline form of dehydrophenylahistin-like compound, and manufacturing and purification method and application thereof

A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.

The present invention provides a myricetin derivative, a preparation method thereof, a pharmaceutical composition containing the same, an application thereof for treating colitis, preventing and treating colitis-associated tumorigenesis and treating colorectal cancer, and an application thereof in preparing a composition for modulating activities of endoplasmic reticulum stress signaling molecules. The myricetin derivative disclosed herein has excellent water solubility, and has biological activities including inhibition of colitis, prevention and treatment of colitis-associated tumorigenesis, and treatment of colorectal cancer. The preparation method disclosed herein uses myricetrin as starting material which is economical and easily available. With the merits of low cost, high yield, high product purity and suitability for large-scale industrial production, the preparation method disclosed herein represents significant market value and economic prospects.

Myricetin derivative and preparing method thereof, and application of same for treating colitis, preventing and treating colitis tumorigenesis, and treating colorectal cancer

Provided are a deuterium-substituted dehydrophenylahistin-like compound, preparation method thereof and use in a preparation of antitumor drugs. The deuterium-substituted dehydrophenylahistin-like compound has a structure of general formula (I), and a synthesis method thereof comprises: firstly conducting a condensation reaction of diacetyldiketopiperazine and an aldehyde intermediate a or a deuterated aldehyde compound b to form a heterocyclic compound c or a deuterium-containing heterocyclic compound d, which is then subjected to a condensation reaction with benzaldehyde and a deuterium-substituted benzaldehyde-like compound to form the deuterium-substituted dehydrophenylahistin-like compound. Also provided are a highly effective deuterated aldehyde intermediate with a high deuterium substitution rate and a deuterium-containing heterocycle intermediate, and a synthesis method thereof. An experiment shows that the deuterium-substituted dehydrophenylahistin-like compound provided by the present invention has an effect on tubulin depolymerization and can treat a refractory solid tumor or lymphoma. The present invention provides a method for researching and developing antitumor drugs of the related compound. 

Deuterated dehydrophenylahistin compounds and preparation method thereof and use thereof in preparation of anti-tumor drugs

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Shandong, China

Shixiao Wang