Category: 1353553-07-7

Li, Si; Wu, Bin; Zheng, Xu; Wang, Changyuan; Zhao, Jingyuan; Sun, Huijun; Sun, Xiuli; Tang, Zeyao; Yuan, Hong; Chen, Lixue; Ma, Xiaodong published an article on January 31 ,2021. The article was titled 《Synthesis and biological activity of imidazole group-substituted arylaminopyrimidines (IAAPs) as potent BTK inhibitors against B-cell lymphoma and AML》, and you may find the article in Bioorganic Chemistry.Synthetic Route of C12H6ClN3O3S The information in the text is summarized as follows:

Bruton’s tyrosine kinase (BTK) is a member of the Tec kinase family and plays a key role in the modulation of the B-cell receptor (BCR)-mediated signaling pathway. Inhibition of BTK has been proven to be an effective therapeutic approach for various hematol. malignancies, such as chronic lymphocytic leukemia (CLL), mantle cell leukemia (MCL), diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML). Here, a new series of imidazole group-substituted arylaminopyrimidines (IAAPs) were designed and synthesized as potent inhibitors of the enzymic activity of BTK with a half maximal inhibitory concentration (IC50) ranging from 13.10 to 42.40 nM. In particular, 11a and 11b exhibited stronger antiproliferative activity against AML and B lymphomas cell lines compared with BTK inhibitor ibrutinib and showed low cytotoxicity against normal peripheral blood mononuclear cells (PBMCs). In addition, anal. of the mechanism of action of these compounds revealed that 11a and 11b induced significant apoptosis in AML and B lymphoma cells by arresting the cell cycle at the G1/G0 or G2/M stage and blocked BTK autophosphorylation as well as the ensuing abrogation of pro-survival AKT and ERK signaling. Taken together, these results suggest that 11a and 11b might serve as valuable preclin. candidates for the treatment of AML and B-cell lymphoma. After reading the article, we found that the author used 2-Chloro-4-(3-nitrophenoxy)thieno[3,2-d]pyrimidine(cas: 1353553-07-7Synthetic Route of C12H6ClN3O3S)

2-Chloro-4-(3-nitrophenoxy)thieno[3,2-d]pyrimidine(cas: 1353553-07-7) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Synthetic Route of C12H6ClN3O3S

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 1353553-07-7On October 1, 2020 ,《Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations》 was published in European Journal of Medicinal Chemistry. The article was written by Xiao, Zhen; Zhou, Zhihui; Chu, Cilong; Zhang, Qian; Zhou, Lingjia; Yang, Zunhua; Li, Xin; Yu, Liying; Zheng, Pengwu; Xu, Shan; Zhu, Wufu. The article contains the following contents:

Five series of novel thiophene-pyrimidine derivatives have been synthesized and tested for their anti-proliferative activity against several cancer cell lines in which EGF is highly expressed. Most of the target compounds showed excellent activity against one or more cancer cell lines. The most promising compound I, of which IC50 values on of cell lines A549 and A431 (4.34 ± 0.60μM and 3.79 ± 0.57μM) were similar to the lead compound Olmutinib, showed strong activity and selectivity to EGFRT790M and EGFRT790M/L858R. Inhibition data of human normal hepatoma cell line LO2 indicated that most target compounds were less toxic to normal cells and had selective inhibitory effects on cancer cells. In addition, the structure-activity relationship was analyzed and the mechanism of apoptosis induced by the compound I was studied. The results showed that compound I induced late apoptosis of A431 cancer cells in a dose-dependent manner. The results came from multiple reactions, including the reaction of 2-Chloro-4-(3-nitrophenoxy)thieno[3,2-d]pyrimidine(cas: 1353553-07-7Application of 1353553-07-7)

2-Chloro-4-(3-nitrophenoxy)thieno[3,2-d]pyrimidine(cas: 1353553-07-7) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Application of 1353553-07-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia