50508-33-3Relevant articles and documents
Diaryl urea compound as well as preparation method and pharmaceutical application thereof
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Paragraph 0053-0056, (2021/05/08)
The invention belongs to the field of medicinal chemistry, and discloses a novel diarylurea compound as shown in a formula (I), physiologically acceptable salts, solvates and crystal forms of the novel diarylurea compound, a preparation method of the comp
Structure-based modification of carbonyl-diphenylpyrimidines (Car-DPPYs) as a novel focal adhesion kinase (FAK) inhibitor against various stubborn cancer cells
Wang, Luhong,Ai, Min,Yu, Jiawen,Jin, Lingling,Wang, Changyuan,Liu, Zhihao,Shu, Xiaohong,Tang, Zeyao,Liu, Kexin,Luo, Hui,Guan, Wenshun,Sun, Xiuli,Ma, Xiaodong
, p. 154 - 162 (2019/04/13)
A family of carbonyl-substituted diphenylpyrimidine derivatives (Car-DPPYs) with strong activity against focal adhesion kinase (FAK), were described in this manuscript. Among them, compounds 7a (IC50 = 5.17 nM) and 7f (IC50 = 2.58 nM) displayed equal anti-FAK enzymatic activity to the lead compound TAE226 (6.79 nM). In particular, compound 7a also exhibited strong antiproliferative activity against several stubborn cancer cells, including AsPC-1 cells (IC50 = 0.105 μM), BxPC-3 cells (IC50 = 0.090 μM), and MCF-7/ADR cells (IC50 = 0.59 μM). Additionally, compound 7a also showed great antitumor efficacy in vivo via aAsPC-1 cancer Xenograft mouse model. The preliminary mechanism study by Western blot analysis revealed that 7a repressed FAK phosphorylation in AsPC cancer cells. Taken together, the results indicate that compound 7a may serve as a promising preclinical candidate for treatment of stubborn cancers.
(E)-3-(Aryl(arylamino)methylene)indolin-2-one derivatives: An efficient synthetic approach and evaluation of their cancer inhibitory activity
Jiang, Hongwu,Feng, Zhiyuan,Chen, Taiping,Li, Zicheng,Huang, Wencai,Luo, Youfu,Zhao, Yinglan
, p. 44 - 49 (2018/02/28)
A series of (E)-3-(aryl(arylamino)methylene)indolin-2-one derivatives were synthesised using an efficient synthetic approach. The method involved reaction of 3-bromo-3-(bromo(aryl)methyl)indolin-2-one with substituted anilines through nucleophilic substitution and a simultaneous elimination using NaHCO3 in DMF. The anticancer activity of the products against four cell lines, HCT-116, A549, SKOV3 and MDA-MB-231, was also evaluated, and several compounds showed moderate inhibitory activity.