Chinese Academy of Sciences

Shanghai Haihe Pharmaceutical Co., Ltd.

Shanghai Nature Standard R&d and Biotech Co., Ltd

Shanghai Standard Technology Co., Ltd.

Shanghai Founder Biomed R&d Co., Ltd.

Jiapeng Li

Yi Chen

Xiang Wang

Linghua Meng

Chunhao Yang

Cun Tan

Yanhong Chen

Jian Ding

Yong Qian

Zhiqin Ji

Xiaoya Zhou

Shaopeng Wei

Tianpei Xie

Disclosed are a use of a methylacryloyl benzimidazolone derivative, an optical isomer or a pharmaceutically acceptable salt or prodrug thereof in the preparation of: (a) a pharmaceutical composition or reagent for down-regulating the activity of PI3K/Akt pathways; (b) a pharmaceutical composition or reagent for treating or inhibiting a tumour; and/or inhibiting tumour cell growth; and/or (c) a pharmaceutical composition or reagent for blocking the cell cycle. The compounds involved in the present invention can down-regulate the level of Akt phosphorylation in P13K/Akt signaling pathways, and the functional effects of the compounds are equivalent to those of a novel small-molecular targeting drug MK2206; while the research at the cellular level has found that the methylacryloyl benzimidazolone derivatives represented by FD1 have a good proliferation inhibiting effect on tumour cells. What is different from MK2206 is that FD1 has better effects on a PTEN deleted cell.

Methylacryloyl benzimidazolone derivative and anti-tumour use thereof

The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.

Pyrrolo[2,1-F[1,2,4]triazine compounds, preparation methods and applications thereof

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Shanghai, China

Jiapeng Li