65190-36-5Relevant academic research and scientific papers
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.
Pyrazole-pyrimido imidazole compound as well as preparation method and application thereof
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Paragraph 0049-0051, (2020/04/22)
The invention relates to a pyrazole-pyrimido imidazole compound as well as a preparation method and application thereof, and belongs to the field of medicinal chemistry and pharmacotherapeutics. The invention provides application of the compound shown in the formula I or the pharmaceutically acceptable salt thereof in preparation of drugs for treating tumor-related diseases.
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.
IRAK INHIBITORS AND USES THEREOF
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Paragraph 00323, (2017/01/26)
The present invention provides compounds, compositions thereof, and methods of using the same for inhibiting one or more interleukin-1 receptor-associated kinases ("IRAK").
CARBOXAMIDE INHIBITORS OF IRAK4 ACTIVITY
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Page/Page column 32, (2016/09/26)
The present invention relates to carboxamide inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors
Zhang, Peilong,Dong, Jiaqiang,Zhong, Boyu,Zhang, Deyi,Yuan, Hongbin,Jin, Can,Xu, Xiangyuan,Li, Hailong,Zhou, Yong,Liang, Zhi,Ji, Minghua,Xu, Tao,Song, Guowei,Zhang, Ling,Chen, Gang,Meng, Xuejing,Sun, Desheng,Shih, Joe,Zhang, Ruihao,Hou, Guojun,Wang, Chengcheng,Jin, Ying,Yang, Qiong
, p. 1910 - 1918 (2016/04/09)
Anaplastic lymphoma kinase (ALK) is a highly attractive therapeutic target for the treatment of some non-small cell lung cancer patients. This Letter describes the further SAR exploration on the novel 3-sulfonylpyrazol-4-amino pyrimidine scaffold. This work identified a compound 53 with very good in vitro/in vivo efficacies, good DMPK properties together with better hERG tolerability and it is currently being profiled for the evaluation as a potential pre-clinical candidate.
HETEROCYCLIC GTP CYCLOHYDROLASE 1 INHIBITORS FOR THE TREATMENT OF PAIN
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Page/Page column 79, (2011/04/19)
The present invention relates to the field of small molecule heterocyclic inhibitors of GTP cyclohydrolase (GCH-I), or a tautomer, prodrug, or pharmaceutically acceptable salt thereof. The invention also features pharmaceutical compositions of the compounds and the medical use of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, or neuropathic pain).
Practical synthesis of novel purine analogues as Hsp90 inhibitors
Semeraro, Teresa,Mugnaini, Claudia,Manetti, Fabrizio,Pasquini, Serena,Corelli, Federico
experimental part, p. 11249 - 11255 (2009/04/06)
The development of a straightforward synthesis of 4-amino-6-benzyl-6H-pyrrolo[3,4-d]pyrimidine and 7-amino-2-benzyl-2H-pyrazolo[4,3-d]pyrimidine derivatives allowed for the preparation of a small family of potential Hsp90 inhibitors. Some of the newly synthesized compounds showed Hsp90 inhibitory activity in preliminary biological assays.
CHEMICAL COMPOUNDS
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Page 131, (2010/02/09)
Quinazoline derivatives of formula (I); for use in the treatment of proliferative diseases such as cancer and in the preparation of medicaments for use in the treatment of proliferative diseases, and to processes for their preparation, as well as pharmaceutical compositions containing them as active ingredient.
