1393900-79-2Relevant academic research and scientific papers
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors
Wang, Yazhou,Huang, Wei,Xin, Minhang,Chen, Pan,Gui, Li,Zhao, Xinge,Tang, Feng,Wang, Jia,Liu, Fei
, p. 75 - 83 (2017)
Janus kinases inhibitor is considered to have therapeutic potential for the treatment of oncology and immune-inflammatory diseases. Two series of 4-(2-benzofuranyl)pyrimidin-2-amine and 4-(4,5,6,7-tetrahydrofuro[3,2-c]pyridin-2-yl)pyrimidin-2-amine derivatives have been designed and synthesized. Primary SAR studies resulted in the discovery of a novel class of 4,5,6,7-tetrahydrofuro[3,2-c]pyridine based JAK2 inhibitors with higher potency (IC50of 0.7 nM) and selectivity (>30 fold) to JAK3 kinase than tofacitinib.
Design, synthesis, and biological evaluation of novel covalent inhibitors targeting focal adhesion kinase
Chen, Lijuan,Chen, Tao,Liu, Yan,Shi, Mingsong,Si, Wenting,Tang, Minghai,Wen, Yi,Yuan, Xue
supporting information, (2021/11/20)
Forty-one new focal adhesion kinase (FAK) covalent inhibitors were designed and synthesized based on FAK inhibitor TAE226. Compound 11w displayed the highest inhibition of FAK with an IC50 value of 35 nM and exhibited potent anticancer activity against Hela, HCT116 and MDA-MB-231 cell lines with IC50 values of 0.41, 0.01 and 0.11 μM respectively, compared to TAE226 (2.68, 0.64 and 4.19 μM respectively). 11w also inhibited the clone formation and migration of HCT-116 cells and stimulated cell cycle arrest in the G2/M phase, inducing tumor cell apoptosis. Compound 11w formed a covalent bond with the Cys427 residue of FAK in a docking model, inhibiting the autophosphorylation of FAK and downstream proteins in a dose-dependent manner. Moreover, 11w showed adequate oral bioavailability of 21.02%. A 74.20% inhibition of tumor growth in the HCT116 xenograft model was also observed. These data indicate that 11w is a promising covalent inhibitor of FAK.
Compound for targeted degradation of adhesion spot kinase and application thereof (by machine translation)
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Paragraph 0079-0081, (2020/11/23)
The invention belongs to the technical field of medicines, and provides a compound as shown in general formula (I) and geometric isomers or pharmaceutically acceptable salts, hydrates, solvates, prodrugs and a preparation method thereof. The compound has good degradation activity on the adhesion spot kinase (FAK). The compounds, and geometric isomers or pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof are as shown in the general formula I, wherein Y, L, X, Z, R1 What is claimed is: the claims and the description. (by machine translation)
BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS
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Page/Page column 108-109, (2017/05/02)
Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.
POTENT DUAL BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS
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Page/Page column 166, (2016/04/26)
Disclosed herein are compounds that are inhibitors of BRD4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BRD4 are also disclosed. In certain aspects, disclosed are compounds of Formula I-IV.
FAK AND FLT3 INHIBITORS
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, (2014/03/22)
The use of a compound of the formula (I): (Formula (I)) in the preparation of a medicament for treating Acute Myeloid Leukemia or a disease ameliorated by the inhibition of Flt3, or Flt3 and FAK.
FAK INHIBITORS
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, (2012/09/10)
A compound of the formula (I): where R1 or R2 is a cycle amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
