1122661-16-8Relevant articles and documents
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
supporting information, 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.
Novel 4-arylaminoquinazoline derivatives with (E)-propen-1-yl moiety as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells
Chen, Li,Zhang, Yaling,Liu, Juan,Wang, Weijia,Li, Xiabing,Zhao, Lijun,Wang, Wei,Li, Baolin
, p. 689 - 697 (2017/07/17)
A series of novel 4-anilinoquinazoline derivatives with (E)-propen-1-yl moiety were designed, synthesized and evaluated for biological activities in vitro. Most compounds exhibited highly antiproliferative activities against all tested tumor cell lines in
Synthesis and biological evaluation of substituted 1,2,3-benzotriazines and pyrido[3,2-d]-1,2,3-triazines as inhibitors of vascular endothelial growth factor receptor-2
Zhao, Xing-Wang,Liu, Dan,Luan, Sheng-Lin,Hu, Guo-Dong,Lv, Jin-Ling,Jing, Yong-Kui,Zhao, Lin-Xiang
, p. 7807 - 7815 (2014/01/06)
A novel series of substituted 1,2,3-benzotriazines and pyrido[3,2-d]-1,2,3- triazines were synthesized. The abilities of these compounds to inhibit the VEGFR-2 kinase activity and the proliferation of human microvascular endothelial cells (MVECs) were det
AROMATIC RING FUSED TRIAZINE DERIVATIVES AND USES THEREOF
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, (2011/08/06)
The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as a
THE AROMATIC RING TRIAZINE DERIVATIVES AND THE USES THEREOF
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Page/Page column 21, (2010/12/01)
The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I. including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as a
Design, synthesis, and antitumor activities of some novel substituted 1,2,3-benzotriazines
Lv, Jin-Ling,Wang, Rui,Liu, Dan,Guo, Gang,Jing, Yong-Kui,Zhao, Lin-Xiang
, p. 1427 - 1440 (2008/12/20)
A series of novel substituted 1,2,3-benzotriazines based on the structures of vatalanib succinate (PTK787) and vandetanib (ZD6474) were designed and synthesized. The antiproliferative effects of these compounds were tested on microvascular endothelial cel