Chinese Academy of Sciences

Zhejiang University

Xiaobei Hu

Yubo Zhou

Jia Tao Li

Tao Liu

Yongzhou Hu

Jia Li

Mingbo Su

Anhui Gao

Xiaowu Dong

Peipei Wang

Pinrao Song

Lexian Tong

Lei Feng

Yu Cheng

Lei Xu

Bo Yang

Xiaohua Chen

Qiaojun He

Weijuan Kan

Yujie Wang

Jiankang Zhang

Huijun Nie

Hongtao Tian

Tian Mi

Kenian Yan

Binshan Zhou

Yuhua Zhong

Gaoya Xu

The present invention relates to a polysubstituted isoindoline compound as shown in general formula (I), and a preparation method, a pharmaceutical composition and the use thereof. In particular, the polysubstituted isoindoline compound is provided in the present invention as a class of novel CRL4E3 ubiquitin ligase modulators in structure, wherein same has a stronger antitumor activity and antitumor spectrum, and can be used to prepare drugs for treating CRL4E3 ligase-related diseases.

Isoindoline compound, preparation method, pharmaceutical composition and use thereof

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

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

Disclosed are a tripeptide epoxyketone compound, a preparation method thereof, and a use thereof in the preparation of anti-tumor drugs.

Tripeptide epoxyketone compound constructed by heterocycle and preparation method and use thereof

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Shanghai, China

Xiaobei Hu