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- Title
Lead compound bearing caffeic scaffold induces EGFR suppression in solid tumor cancer cells.
- Authors
Mudjupa, Chawannuch; Abdelhamed, Sherif; Refaat, Alaa; Yokoyama, Satoru; Saiki, Ikuo; Vajragupta, Opa
- Abstract
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 IC 50 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 IC 50 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.
- Subjects
CANCER cell growth; CAFFEIC acid; EPIDERMAL growth factor receptors; BREAST cancer; ANTINEOPLASTIC agents; PREVENTION
- Publication
Journal of Applied Biomedicine, 2015, Vol 13, Issue 4, p305
- ISSN
1214-021X
- Publication type
Article
- DOI
10.1016/j.jab.2015.05.001