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Mostafa M. Ghorab Mansour S. Alsaid Aiten M. Soliman Abdullah A. Al-Mishari 《Journal of enzyme inhibition and medicinal chemistry》2018,33(1):67-73
Targeting EGFR has proven to be beneficial in the treatment of several types of solid tumours. So, a series of novel 2-(4-oxo-3-(4-sulfamoylphenyl)-3,4-dihydrobenzo[g]quinazolin-2-ylthio)-N-substituted acetamide 5–19 were synthesised from the starting material 4-(2-mercapto-4-oxobenzo[g]quinazolin-3(4H)-yl) benzenesulfonamide 4, to be evaluated as dual EGFR/HER2 inhibitors. The target compounds 5–19, were screened for their cytotoxic activity against A549 lung cancer cell line. The percentage inhibition of EGFR enzyme was measured and compared with erlotinib as the reference drug. Compounds 6, 8, 10, and 16 showed excellent EGFR inhibitory activity and were further selected for screening as dual EGFR/HER2 inhibitors. The four selected compounds showed IC50 ranging from 0.009 to 0.026?µM for EGFR and 0.021 to 0.069?µM for the HER2 enzyme. Compound 8 was found to be the most potent in this study with IC50 0.009 and 0.021?µM for EGFR and HER2, respectively. 相似文献
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Nasr Fahd A. Shahat Abdelaaty A. Alqahtani Ali S. Ahmed Mohammad Z. Qamar Wajhul Al-Mishari Abdullah A. Almoqbil Abdulaziz N. 《Molecular biology reports》2020,47(8):6043-6051
Molecular Biology Reports - Centaurea bruguierana, of the Asteraceae family, has a long history of use in traditional medicines for the treatment of various ailments. However, the anticancer... 相似文献
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