61032-42-6Relevant articles and documents
Method for preparing vanonitinib and analogue intermediate thereof through electro-reduction
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Paragraph 0078-0085, (2021/03/18)
The invention relates to an electroreduction preparation method of 2-amino-5-methoxybenzoic acid derivatives represented by a formula I shown in the specification. A preparation reaction is shown in the specification, wherein n is selected from 1, 2 or 3;
Design and discovery of 4-anilinoquinazoline-urea derivatives as dual TK inhibitors of EGFR and VEGFR-2
Zhang, Hai-Qi,Gong, Fei-Hu,Ye, Ji-Qing,Zhang, Chi,Yue, Xiao-Hong,Li, Chuan-Gui,Xu, Yun-Gen,Sun, Li-Ping
, p. 245 - 254 (2016/10/03)
EGFR and VEGFR-2 are involved in pathological disorders and the progression of different kinds of tumors, the combined blockade of EGFR and VEGFR signaling pathways appears to be an attractive approach to cancer therapy. In this work, a series of 4-anilinoquinazoline derivatives containing substituted diaryl urea or glycine methyl ester moiety were designed and identified as EGFR and VEGFR-2 dual inhibitors. Compounds 19i, 19j and 19l exhibited the most potent inhibitory activities against EGFR (IC50?=?1?nM, 78?nM and 51?nM, respectively) and VEGFR-2 (IC50?=?79?nM, 14?nM and 14?nM, respectively), they showed good antiproliferative activities as well. Molecular docking established the interaction of 19i with the DFG-out conformation of VEGFR-2, suggesting that they might be type II kinase inhibitors.
Epidermal growth factor receptor tyrosine kinase inhibitors MPGF and MPGH with anti-tumor activity and preparation method and application thereof
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Paragraph 0044; 0047, (2016/10/27)
The invention discloses epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKI) MPGF and MPGH with the anti-tumor activity and a preparation method and application thereof. By optimizing and improving the chemical structure of PD153035, brand-new EGFR TKIs are obtained and named as MPGF (shown in the formula I) and MPGH (shown in the formula II). Research shows that the synthesized EGFR TKI-MPGF and EGFR TKI-MPGH can effectively inhibit tumor cell proliferation and has a stronger proliferation inhibition effect on mutational EGFR lung cancer cell line PC-9 compared with the PD153035, and therefore the EGFR TKI-MPGF and the EGFR TKI-MPGH can serve as anti-tumor agents to be applied in clinic. In addition, the invention discloses the method for preparing the epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKI) MPGF and MPGH with the anti-tumor activity. By means of the epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKI) MPGF and MPGH with the anti-tumor activity and the preparation method and application thereof, an effective technological means is provided for tumor treatment, especially for treatment of the non-small cell lung cancer.