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Lead compound bearing caffeic scaffold induces EGFR suppression in solid tumor cancer cells
Chawannuch Mudjupa, Sherif Abdelhamed, Alaa Refaat, Satoru Yokoyama, Ikuo Saiki, Opa Vajragupta
Jazyk angličtina Země Česko
Typ dokumentu hodnotící studie, práce podpořená grantem
- MeSH
- erbB receptory antagonisté a inhibitory chemie MeSH
- kyseliny kávové chemie MeSH
- metastázy nádorů MeSH
- molekulární modely MeSH
- molekulární sondy - techniky MeSH
- nemalobuněčný karcinom plic farmakoterapie MeSH
- proliferace buněk MeSH
- triple-negativní karcinom prsu farmakoterapie MeSH
- Publikační typ
- hodnotící studie MeSH
- práce podpořená grantem MeSH
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.
Citace poskytuje Crossref.org
Literatura
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- $a Mudjupa, Chawannuch $u Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudya Road, Bangkok 10400, Thailand
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- $a Lead compound bearing caffeic scaffold induces EGFR suppression in solid tumor cancer cells / $c Chawannuch Mudjupa, Sherif Abdelhamed, Alaa Refaat, Satoru Yokoyama, Ikuo Saiki, Opa Vajragupta
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- $a 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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- $a Abdelhamed, Sherif $u Division of Pathogenic Biochemistry, Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan $7 gn_A_00000326
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- $a Vajragupta, Opa $u Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudya Road, Bangkok 10400, Thailand; Center of Excellence for Innovation in Drug Design and Discovery, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudya Road, Bangkok 10400, Thailand
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