1582283-80-4Relevant academic research and scientific papers
Discovery of new HER2/EGFR dual kinase inhibitors based on the anilinoquinazoline scaffold as potential anti-cancer agents
Sadek, Maiada M.,Serrya, Rabah A.,Kafafy, Abdel-Hamid N.,Ahmed, Marawan,Wang, Feng,Abouzid, Khaled A. M.
, p. 215 - 222 (2014)
Herein, we designed and synthesized certain anilinoquinazoline derivatives bearing bulky arylpyridinyl, arylpropenoyl and arylpyrazolyl moieties at the 4′ position of the anilinoquinazoline, as potential dual HER2/EGFR kinase inhibitors. A detailed molecular modeling study was performed by docking the synthesized compounds in the active site of the epidermal growth factor receptor (EGFR). The synthesized compounds were further tested for their inhibitory activity on EGFR and HER2 tyrosine kinases. The aryl 2-imino-1,2-dihydropyridine derivatives 5d and 5e displayed the most potent inhibitory activity on EGFR with IC50 equal to 2.09 and 1.94 μM, respectively, and with IC50 equal to 3.98 and 1.04 μM on HER2, respectively. Furthermore, the anti-proliferative activity of these most active compounds on MDA-MB-231 breast cancer cell lines, known to overexpress EGFR, showed an IC50 range of 2.4 and 2.5 μM, respectively.
Chalcone phosphonate derivative containingquinazoline and preparation method and application of chalcone phosphonate derivative
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Paragraph 0023; 0029; 0058, (2016/10/09)
The invention discloses a chalcone phosphonate derivative containingquinazoline and a preparation method and application of the chalcone phosphonate derivative. The structural formula (1) of the chalcone phosphonate derivative is as shownin thespecification, and in the formula, R1 is phenyl, 3-bromophenyl, 2-chlorophenyl, 4-bromophenyl, 2-fluorophenyl, 2-thienyl, 2,6-dichlorophenyl, 4-chlorophenyl, 2-furyl, 2-trifluoromethylphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-chloro-6-fluorophenyl. The chalcone phosphonate derivative is simple in synthesis route, high in yield and capable of efficiently and safely preventing and treating plant virus diseases.
