کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2087665 | 1080679 | 2015 | 13 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Lead compound bearing caffeic scaffold induces EGFR suppression in solid tumor cancer cells Lead compound bearing caffeic scaffold induces EGFR suppression in solid tumor cancer cells](/preview/png/2087665.png)
• CIU1 was identified as novel lead compound for anticancer drug development.
• CIU1 was designed in silico by using a privilege scaffold from natural sources.
• CIU1 inhibited the growth of EGFR-overexpressing TNBC and NSCLC cells.
• CIU1 effectively inhibited the invasive hormone-dependent MCF-7 cancer cells.
• CIU1 suppressed EGFR expression and induced programmed cell death.
A small molecule EGFR inhibitor, 4-(2-(3-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)ureido)vinyl)-1,2-phenylene diacetate (CIU1) was designed in silico by using caffeic scaffold as core structure. The designed compound showed anti-proliferative action against different solid tumor cell lines, particularly metastatic breast cancer cells. CIU1 inhibited the growth of EGFR-overexpressing MDA-MB-468 triple-negative breast cancer cells and wild-type non-small-cell lung cancer H460 cells with IC50 values of 8.96 μM and 12.98 μM, respectively, these anti-proliferative effects of CIU1 were comparable to gefitinib (a specific EGFR inhibitor) or lapatinib (a dual EGFR and HER2 tyrosine kinase inhibitor). Interestingly CIU1 effectively inhibited the invasive hormone-dependent MCF-7 cancer cells with an IC50 2.34 μM. The immunoblot analyses revealed that CIU1 induced programmed cell death and suppressed EGFR expression in EGFR-overexpressing breast cancer (MDA-MB468) and lung cancer (PC-9) cells. The findings substantiated our design strategy and demonstrated the potential of CIU1 as new lead for further optimization in the development of anticancer drugs against advanced solid tumors.
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Journal: Journal of Applied Biomedicine - Volume 13, Issue 4, November 2015, Pages 305–317