Chinese Academy of Sciences

Other

Suzhou Baijibugong Pharmaceutical Technology Co., Ltd.

Zibo Biopolar Changsheng Pharmaceutical Co. Ltd.

Zhejiang University

Anhui Gao

Jia Tao Li

Yubo Zhou

Zhijian Lu

Xibin Liao

Jia Li

Mingbo Su

Yongzhou Hu

Tao Liu

Xiaobei Hu

Peipei Wang

Xiaowu Dong

Lexian Tong

Pinrao Song

Jian Ding

Yi Chen

Meiyu Geng

Fajun Nan

Yangming Zhang

Chaojun Gong

Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):

Bruton's tyrosine kinase inhibitors

The present invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof, the compound, and an optical isomer thereof or a pharmaceutically thereof acceptable salts or solvates can be used in the preparation of anti-tumor drugs. The invention designs and synthesizes a series of novel small molecule Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained by structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess potent anticancer activity, Chk1 kinase inhibitory activity, and are promising Chk1 inhibitors, and can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal. The 2-polysubstituted aromatic ring-pyrimidine derivatives provided by the present invention has the structure of the formula I: 

2-polysubstituted aromatic ring-pyrimidine derivatives, preparation and medical application thereof

Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I): 

A 2-substituted aromatic ring-pyrimidine derivative as shown in a general formula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chk1 kinase inhibitory activity and are promising Chk1 inhibitors. The compounds can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal.

2-substituted aromatic ring-pyrimidine derivative and preparation and application thereof

The invention describes an aryl-2,2'-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2&#x2032;-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs. 

Aryl-2,2'-tandem bisthiazole compound and preparation method and use thereof

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Shanghai, China

Anhui Gao