141060-00-6Relevant articles and documents
Linifanib-a multi-targeted receptor tyrosine kinase inhibitor and a low molecular weight gelator
Marlow, Maria,Al-Ameedee, Mohammed,Smith, Thomas,Wheeler, Simon,Stocks, Michael J.
, p. 6384 - 6387 (2015)
In this study we demonstrate that linifanib, a multi-targeted receptor tyrosine kinase inhibitor, with a key urea containing pharmacophore, self-assembles into a hydrogel in the presence of low amounts of solvent. We demonstrate the role of the urea functional group and that of fluorine substitution on the adjacent aromatic ring in promoting self-assembly. We have also shown that linifanib has superior mechanical strength to two structurally related analogues and hence increased potential for localisation at an injection site for drug delivery applications. This journal is
Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation
Xu, Dandan,Sun, Deqiao,Wang, Wei,Peng, Xia,Zhan, Zhengsheng,Ji, Yinchun,Shen, Yanyan,Geng, Meiyu,Ai, Jing,Duan, Wenhu
, (2021/05/06)
Axl has emerged as an attractive target for cancer therapy due to its strong correlation with tumor growth, metastasis, poor survival, and drug resistance. Herein, we report the design, synthesis and structure-activity relationship (SAR) investigation of a series of pyrrolo[2,3-d]pyrimidine derivatives as new Axl inhibitors. Among them, the most promising compound 13b showed high enzymatic and cellular Axl potencies. Furthermore, 13b possessed preferable pharmacokinetic properties and displayed promising therapeutic effect in BaF3/TEL-Axl xenograft tumor model. Compound 13b may serve as a lead compound for new antitumor drug discovery.
Method for preparing acyl chloride by catalyzing phosgene and acid
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Paragraph 0055; 0056; 0057, (2016/10/20)
The invention discloses a method for preparing acyl chloride by catalyzing phosgene and acid. The method includes the following steps that 1, with carboxylic acid as a raw material, a catalyst and a solvent are added, and under the condition that the temperature is maintained to range from 20 DEG C to 200 DEG C, phosgene is introduced into a reaction flask for a reaction; 2, after the molar ratio of carboxylic acid to phosgene reaches 1:1.0-1:10, phosgene introduction is stopped, reacted mixed liquor is obtained and filtered, obtained filter liquor is subjected to reduced pressure distillation at a high vacuum degree to obtain acyl chloride, and an obtained filter cake continues to serve as the catalyst in the step 1 to be recycled. Compared with an existing catalyst adopted for preparing acyl chloride according to a phosgene method, the catalyst used in the method is small in dosage, convenient to recycle, easy to separate from a product, better in product quality, safe, stable and environmentally friendly, generated solid waste is greatly reduced, the experience of operators is greatly improved, and safety risks are lowered.