912556-91-3Relevant academic research and scientific papers
Synthesis and biological evaluation of selenogefitinib for reducing bleomycin-induced pulmonary fibrosis
Bai, Yue,Zhang, Yunhao,Chu, Peng,Wang, Changyuan,Li, Lei,Qi, Yan,Han, Xu,Zhang, Baojing,Sun, Huijun,Li, Yanxia,Chen, Lixue,Ma, Xiaodong
, (2021/07/08)
Selenium has demonstrated effectiveness in the reduction of oxidative stress and inflammation in vitro and in vivo, both of which are key indicators of the pathogenesis of pulmonary fibrosis. Gefitinib, an FDA-approved EGFR inhibitor, effectively reverses
Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and α-glucosidase
Zhang, Yaling,Gao, Hongliang,Liu, Renjie,Liu, Juan,Chen, Li,Li, Xiabing,Zhao, Lijun,Wang, Wei,Li, Baolin
, p. 4309 - 4313 (2017/09/12)
A series of novel quinazoline-1-deoxynojirimycin hybrids were designed, synthesized and evaluated for their inhibitory activities against two drug target enzymes, epidermal growth factor receptor (EGFR) tyrosine kinase and α-glucosidase. Some synthesized compounds exhibited significantly inhibitory activities against the tested enzymes. Comparing with reference compounds gefitinib and lapatinib, compounds 7d, 8d, 9b and 9d showed higher inhibitory activities against EGFR (IC50: 1.79–10.71 nM). Meanwhile the inhibitory activities of 7d, 8d and 9c against α-glucosidase (IC50 = 0.14, 0.09 and 0.25 μM, respectively) were obvious higher than that of miglitol (IC50 = 2.43 μM), a clinical using α-glucosidase inhibitor. Interestingly, compound 9d as a dual inhibitor showed high inhibitory activity to EGFRwt tyrosine kinase (IC50 = 1.79 nM), also to α-glucosidase (IC50 = 0.39 μM). The work could be very useful starting point for developing a new series of enzyme inhibitors targeting EGFR and/or α-glucosidase.
N '-aryl-N, N-dimethyl-formamidine new method for the preparation of (by machine translation)
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Paragraph 0085-0087, (2017/02/17)
The present invention provides a synthetic N '-aryl-N, N-dimethyl-formamidine of the new method. The method firstly to N, N-dimethyl formamide and dimethyl sulfate to imine salt; generating imide salt in the presence of an alkali, and aromatic amine reaction generating N '-aryl-N, N-dimethyl-carboximidamide; the amidines same with other amine function generating [...] compound, can be used in the anti-tumor drug AKT, synthesis of lapatinib and gefitinib, and the like. Mild reaction conditions of the method, is suitable for industrial production. (by machine translation)
AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE
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Paragraph 0277-0278, (2014/08/19)
The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
Heterocycle Amido Alkyloxy Substituted Quinazoline Derivative and Use Thereof
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Paragraph 0225; 0229, (2014/08/06)
Heterocycle amino alkyloxy substituted quinazoline derivatives as represented by the structural Formula (I) and pharmaceutically acceptable salts thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family are provided.
HETEROCYCLE AMIDO ALKYLOXY SUBSTITUTED QUINAZOLINE DERIVATIVE AND USE THEREOF
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Paragraph 0082, (2014/11/13)
Heterocycle amino alkyloxy substituted quinazoline derivatives as represented by the structural Formula (I) and pharmaceutically acceptable salts thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family are provided.
AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE
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Paragraph 00197, (2013/06/05)
The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter-and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
Four-membered heterocycles-containing 4-anilino-quinazoline derivatives as epidermal growth factor receptor (EGFR) kinase inhibitors
Zhao, Feng,Lin, Zhaohu,Wang, Feng,Zhao, Weili,Dong, Xiaochun
, p. 5385 - 5388 (2013/09/23)
We report herein the design and synthesis of novel azaspirocycle or azetidine substituted 4-anilinoquinazoline derivatives. The EGFR inhibitory activities and in vitro antitumor potency of these newly synthesized compounds against two lung cancer cell lines HCC827 and A549 were evaluated. Most of the target compounds possess good inhibitory potency. In particular, compounds 21g with 2-oxa-6-azaspiro[3.4]octane substituent was found to possess higher EGFR inhibitory activities and similar antitumor potency comparing to the lead compound gefitinib with improved water solubility.
Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines
Li, Ri-Dong,Zhang, Xin,Li, Qiao-Yan,Ge, Ze-Mei,Li, Run-Tao
, p. 3637 - 3640 (2011/08/06)
On the basis of combination strategy, a novel series of EGFR inhibitors were designed and synthesized by combination of dithiocarbamic acid esters and 4-anilinoquinazolines. The effect of the synthesized compounds on cell proliferation was evaluated by MTT assay in three human cancer cell lines: MDA-MB-468, SK-BR-3 and HCT-116. Two compounds (11d and 11f) were found more potent against all three cell lines and five compounds (11a, 11d-11g) were found more potent against both MDA-MB-468 and SK-BR-3 than Lapatinib. SAR studies revealed that the substituents on C6 and C7 positions of quinazoline, the amine component of dithiocarbamate moiety and the linker greatly affected the activity. This work provides a promising new strategy for the preparation of potent tyrosine kinase inhibitors.
Synthesis of gefitinib from methyl 3-hydroxy-4-methoxy-benzoate
Ming, Dong Li,You, Guang Zheng,Ji, Min
, p. 673 - 678 (2008/02/01)
This paper reports a novel synthesis of gefitinib starting from methyl 3-hydroxy-4-methoxybenzoate. The process starts with alkylation of the starting material, followed by nitration, reduction, cyclization, chlorination and two successive amination reactions. The intermediates and target molecule were characterized by 1H-NMR, 13C-NMR, MS and the purities of all these compounds were determined by HPLC. This novel synthetic route produced overall yields as high as 37.4%.
