Discovery of anilino-furo [2, 3-d] pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity
M Hossam, DS Lasheen, NSM Ismail, A Esmat… - European Journal of …, 2018 - Elsevier
Being responsible for the development of many cancer types, EGFR (Epidermal Growth
Factor Receptor) and HER2 (Human Epidermal growth factor Receptor 2) were the focus of …
Factor Receptor) and HER2 (Human Epidermal growth factor Receptor 2) were the focus of …
Design and Synthesis of 4‐Anilinothieno[2,3‐d]pyrimidine‐Based Compounds as Dual EGFR/HER‐2 Inhibitors
Dual inhibition of the epidermal growth factor receptor (EGFR) and the human epidermal
growth factor receptor 2 (HER‐2) is an attractive cancer therapeutic approach. In this study …
growth factor receptor 2 (HER‐2) is an attractive cancer therapeutic approach. In this study …
Design, synthesis and anticancer evaluation of thieno [2, 3-d] pyrimidine derivatives as dual EGFR/HER2 inhibitors and apoptosis inducers
SA Elmetwally, KF Saied, IH Eissa, EB Elkaeed - Bioorganic chemistry, 2019 - Elsevier
Deregulation of many kinases is directly linked to cancer development and the tyrosine
kinase family is one of the most important targets in current cancer therapy regimens. In this …
kinase family is one of the most important targets in current cancer therapy regimens. In this …
Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy) anilino]-6-(3-substituted-phenoxy) pyrimidines as dual EGFR/ErbB-2 kinase inhibitors
S Li, C Guo, H Zhao, Y Tang, M Lan - Bioorganic & medicinal chemistry, 2012 - Elsevier
A series of 4-[3-chloro-4-(3-fluorobenzyloxy) anilino]-6-(3-substituted-phenoxy) pyrimidine
derivatives were elaborately designed based on the skeleton of Lapatinib, and evaluated for …
derivatives were elaborately designed based on the skeleton of Lapatinib, and evaluated for …
Discovery of a novel class anti-proliferative agents and potential inhibitors of EGFR tyrosine kinases based on 4-anilinotetrahydropyrido [4, 3-d] pyrimidine scaffold …
Y Zhang, K Zhang, M Zhao, L Zhang, M Qin… - Bioorganic & Medicinal …, 2015 - Elsevier
A novel series of 4-arylamino-6/7-substituted-5, 6, 7, 8-tetrahydropyrido [4, 3-d] pyrimidines
were designed, synthesized and their biological activities as the potential anti-proliferative …
were designed, synthesized and their biological activities as the potential anti-proliferative …
Design and synthesis of pyrrolo [3, 2-d] pyrimidine HER2/EGFR dual inhibitors: Improvement of the physicochemical and pharmacokinetic profiles for potent in vivo …
Y Kawakita, K Miwa, M Seto, H Banno, Y Ohta… - Bioorganic & medicinal …, 2012 - Elsevier
During the course of our studies on a novel HER2/EGFR dual inhibitor (TAK-285), we found
an alternative potent pyrrolo [3, 2-d] pyrimidine compound (1a). To enhance the …
an alternative potent pyrrolo [3, 2-d] pyrimidine compound (1a). To enhance the …
Novel inhibitors of epidermal growth factor receptor:(4-(Arylamino)-7H-pyrrolo [2, 3-d] pyrimidin-6-yl)(1H-indol-2-yl) methanones and (1H-indol-2-yl)(4-(phenylamino) …
T Beckers, A Sellmer, E Eichhorn, H Pongratz… - Bioorganic & medicinal …, 2012 - Elsevier
Several members of the quinazoline class of known tyrosine kinase inhibitors are approved
anticancer agents, often showing selectivity for receptors of the HER/ErbB-family. Combining …
anticancer agents, often showing selectivity for receptors of the HER/ErbB-family. Combining …
Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase …
Y Mao, W Zhu, X Kong, Z Wang, H Xie, J Ding… - Bioorganic & medicinal …, 2013 - Elsevier
36 new compounds with the typical skeleton of 4-anilino-5-vinyl/ethynyl pyrimidine, 4-anilino-
3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed …
3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed …
Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors
TR Rheault, TR Caferro, SH Dickerson… - Bioorganic & medicinal …, 2009 - Elsevier
Two new series of potent and selective dual EGFR/ErbB-2 kinase inhibitors derived from
novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were …
novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were …
Discovery of new thieno[2,3-d]pyrimidines as EGFR tyrosine kinase inhibitors for cancer treatment
Background: EGFR has been considered a vital molecular target in cancer management.
Aim: The discovery of new thieno [2, 3-d] pyrimidine derivatives as EGFR tyrosine kinase …
Aim: The discovery of new thieno [2, 3-d] pyrimidine derivatives as EGFR tyrosine kinase …
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