906565-52-4Relevant academic research and scientific papers
QUINAZOLINE COMPOUND SERVING AS EGFR TRIPLE MUTATION INHIBITOR AND APPLICATIONS THEREOF
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Paragraph 0060-0061, (2021/02/18)
Related to a quinazoline compound serving as an EFGR triple mutation inhibitor and applications thereof. Specifically, disclosed are a compound as represented by the following formula (I), a pharmaceutical composition comprising the compound of formula (I
Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFRL858R/T790M/C797S
Li, Qiannan,Zhang, Tao,Li, Shiliang,Tong, Linjiang,Li, Junyu,Su, Zhicheng,Feng, Fang,Sun, Deheng,Tong, Yi,Wang, Xia,Zhao, Zhenjiang,Zhu, Lili,Ding, Jian,Li, Honglin,Xie, Hua,Xu, Yufang
supporting information, p. 869 - 873 (2019/06/08)
In this paper, we describe the discovery and optimization of a series of noncovalent reversible epidermal growth factor receptor inhibitors of EGFRL858R/T790M/C797S. One of the most promising compounds, 25g, inhibited the enzymatic activity of EGFRL858R/T790M/C797S with an IC50 value of 2.2 nM. Cell proliferation assays showed that 25g effectively and selectively inhibited the growth of EGFRL858R/T790M/C797S-dependent cells. This series of compounds, which occupy both the ATP binding site and the allosteric site of the EGFR kinase, may serve as a basis for the development of fourth-generation EGFR inhibitors for L858R/T790M/C797S mutants.
Fluorine-18 labeling of 6,7-disubstituted anilinoquinazoline derivatives for positron emission tomography (PET) imaging of tyrosine kinase receptors: Synthesis of18F-Iressa and related molecular probes
Seimbille, Yann,Phelps, Michael E.,Czernin, Johannes,Silverman, Daniel H. S.
, p. 829 - 843 (2007/10/03)
Inhibitors of tyrosine kinase enzymatic activity represent a promising new class of antineoplastic agents. Although clinical studies performed over the last decade give more insight on the potential therapeutic applications of such drugs, identification of the individual patients who might benefit from them remains a major challenge. We have developed a synthetic strategy for the production of a wide variety of radiolabeled 6,7-disubstituted 4-anilinoquinazolines suitable for noninvasive imaging of tyrosine kinase receptors to predict therapy effectiveness. Three new F-18 labeled radiopharmaceuticals based on the therapeutic agents Tarceva, Iressa, and ZD6474 were synthesized. Decay-corrected yields varied between 25 and 40% for a total synthesis time of 120 min, thus providing F-18 labeled tyrosine kinase inhibitors in quantities and times practical for use as PET radiopharmaceuticals. Copyright
Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity
Boschelli, Diane H.,Ye, Fei,Wu, Biqi,Wang, Yanong D.,Barrios Sosa, Ana Carolina,Yaczko, Deanna,Powell, Dennis,Golas, Jennifer M.,Lucas, Judy,Boschelli, Frank
, p. 3797 - 3800 (2007/10/03)
Several 7-alkoxy-4-anilino-3-quinolinecarbonitriles were synthesized and evaluated for Src kinase inhibitory activity. Optimal inhibition of both Src enzymatic and cellular activity was seen with analogues having a 2,4-dichloro-5-methoxyaniline group at C-4. Compound 18, which has a 1-methylpiperidinemethoxy group at C-7, showed in vivo activity in a xenograft model.
