162012-71-7Relevant articles and documents
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor
Zhang, Xu,Peng, Ting,Ji, Xun,Li, Jian,Tong, Linjiang,Li, Zeng,Yang, Wei,Xu, Yungen,Li, Mengyuan,Ding, Jian,Jiang, Hualiang,Xie, Hua,Liu, Hong
, p. 7988 - 7998 (2013)
A novel series of anilinoquinazoline compounds with C-6 urea-linked side chains was designed and synthesized as reversible inhibitors of epidermal growth factor receptor (EGFR) based on the structure-activity relationships (SARs) of anilinoquinazoline inhibitors. All compounds demonstrated good inhibition of EGFR wild type (EGFR wt) (IC50 = 0.024-1.715 μM) and inhibited proliferation of A431cell line (IC50 = 0.116-22.008 μM). The binding mode of compounds 8a, 8d, 8k and 8o was consistent with the biological results. Moreover, compounds 8k and 8l almost completely blocked the phosphorylation of EGFR in A431 cell line at 0.01 μM. Interestingly, all of the compounds also demonstrated moderate inhibition of EGFR/T790M/L858R (IC 50 = 0.049-5.578 μM). In addition, compounds 8f and 8h blocked the autophosphorylation of EGFR in NCI-H1975 cells at high concentration (10 μM), and compound 8f was confirmed to be an irreversible inhibitor through the dilution method. Importantly, the compounds with C-6 urea-linked side chains which did not contain Michael acceptors demonstrated moderate to strong irreversible EGFR inhibition.
Benzo nitrogen hetero-aromatic ring compound, and preparation method and applications thereof
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Paragraph 0301; 0302; 0303; 0304, (2018/03/01)
The invention belongs to the field of chemical medicine, and discloses a benzo nitrogen hetero-aromatic ring compound represented by formula I, or pharmaceutically acceptable salts, stereisomers, racemic compounds, prodrugs, or solvates thereof. The invention also discloses applications of the benzo nitrogen hetero-aromatic ring compound in preparation of drugs used for treating diseases caused byprotein kinase and/or nicotinamide phosphoribosyltransferase abnormal activity. The benzo nitrogen hetero-aromatic ring compound represented by formula I or the salts thereof possess tyrosine kinaseand Nampt double inhibition effects, can be taken as effective components in treatment or prevention of tumor, are excellent in curative effect, and low in toxic or side effect.
Artemisin derivative and its preparation and use
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Paragraph 0303; 0304; 0308, (2016/10/08)
Provided are artemisinin derivatives of formula (I) or pharmaceutically acceptable salts thereof, or enantiomers, diastereomers, and racemic bodies thereof, and a pharmaceutical composition of the compounds, the preparation process and uses thereof. Artemisinin derivatives of formula (I) have excellent effects in the treatment of tumours.
