1089279-90-2Relevant articles and documents
Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing a sulfoxide moiety as anaplastic lymphoma kinase (ALK) inhibition agents
Wu, Feng,Yao, Han,Li, Wei,Zhang, Niuniu,Fan, Yangyang,Chan, Albert S.C.,Li, Xingshu,An, Baijiao
, (2021/07/19)
Anaplastic lymphoma kinase (ALK) targeted therapies have demonstrated remarkable efficacy in ALK-positive lung adenocarcinomas. Here we synthesized and evaluated sixteen new 2,4-diaminopyrimidines bearing a sulfoxide moiety as anaplastic lymphoma kinase (ALK) inhibitors. The optimal compound 9e exhibited excellent antiproliferative activity against non-small cell lung cancer NCI-H2228 cells, which is better than that of Brigatinib and similar to Ceritinib. Mechanism study revealed that the optimal compound 9e decreased the mitochondrial membrane potential and arrested NCI-H2228 cells in the G0/G1 phase, finally resulting in cellular apoptosis. It is interesting that 9e could effectively inhibit the migration of NCI-H2228 cells and may be a promising leading compound for chemotherapy of metastatic cancer.
PYRIMIDINE DERIVATIVE AND USE THEREOF
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Paragraph 0261; 0262; 0263, (2018/09/27)
The present invention provides a pyrimidine derivative and a use thereof. The pyrimidine derivative is the compound shown in formula I or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein, R1, R2, R3, R4 and R5 are, for example, as defined in the specification. The compound can act as an ALK inhibitor, and is for preparing an anti-tumor medicament for suppressing an anaplastic lymphoma kinase.
NOVEL CHEMICAL COMPOUNDS (VARIANTS) AND THE USE THEREOF TO TREAT ONCOLOGICAL DISEASES
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Paragraph 0304; 0305, (2016/10/08)
The invention relates to novel chemical compounds of general formula I, in which L A , L B , L C , ring A, ring B, R A , R B , R C ,R D ,R E and R F have are defined in the description, and which are protein kinases inhibitors. The invention also relates