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Lead compound bearing caffeic scaffold induces EGFR suppression in solid tumor cancer cells
Mudjupa C. - ไม่ระบุหน่วยงาน
ชื่อเรื่อง (EN): Lead compound bearing caffeic scaffold induces EGFR suppression in solid tumor cancer cells
ผู้แต่ง / หัวหน้าโครงการ (EN): Mudjupa C.
บทคัดย่อ (EN): 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. © 2015 Faculty of Health and Social Studies, University of South Bohemia in Ceske Budejovice. Published by Elsevier Sp. z o.o. All rights reserved.
บทคัดย่อ: ไม่พบข้อมูลจากหน่วยงานต้นทาง
ภาษา (EN): en
เอกสารแนบ (EN): https://www.scopus.com/inward/record.uri?eid=2-s2.0-84969664314&doi=10.1016%2fj.jab.2015.05.001&partnerID=40&md5=bfd24f029c30fb47776caddfd34d9b1e
เผยแพร่โดย (EN): มหาวิทยาลัยมหิดล
คำสำคัญ (EN): MCF 7 cell line
เจ้าของลิขสิทธิ์ (EN): มหาวิทยาลัยมหิดล
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Lead compound bearing caffeic scaffold induces EGFR suppression in solid tumor cancer cells
Mudjupa C.
มหาวิทยาลัยมหิดล
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