65190-36-5Relevant articles and documents
Design, synthesis, and cytotoxic activity of novel 2H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidine derivatives
Zheng, You-Guang,Pei, Xin,Xia, De-Xin,Wang, Yuan-Bo,Jiang, Ping,An, Lin,Huang, Tong-Hui,Xue, Yun-Sheng
, (2021/02/26)
In this study, a series of novel 2H-imidazo [1, 2-c] pyrazolo [3, 4-e] pyrimidine derivatives were designed, synthesized, and evaluated for their cytotoxic activities. The in vitro cell growth inhibition assay of the target compounds indicated their selectivity in inhibiting the proliferation of blood tumor cells (K562, U937) and solid tumor cells (HCT116, HT-29). Compound 9b exhibited the highest antiproliferative activities against K562 (IC50 = 5.597 μM) and U937 (IC50 = 3.512 μM). Based on the flow cytometry assays, compound 9b caused obvious induction of cell apoptosis and cell arrest at the S phase. Furthermore, western blot analysis revealed that compound 9b upregulated the expression of Bax, downregulated the levels of Bcl-2, and further activated caspase-3 in K562 cells. Therefore, compound 9b may be a potential anticancer agent that deserves further investigation.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 2365; 2366, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
ALK KINASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0378; 0381; 0382, (2017/04/18)
An ALK kinase inhibitor compound as represented by Formula I, pharmaceutical composition containing the compound, and preparation method and use thereof in the preparation of drugs serving as an ALK inhibitor for treating cancer.