EGFR 과발현 세포인 A431과 MDA-MB-468에 대한 1-옥소-1,2,3,4- 테트라하이드로피라지노[1,2-a]인돌-3-카르복사마이드 유도체의 항암 활성

Anticancer Activity of 1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-3-carboxamide analogs against A431 and MDA-MB-468 cell lines overexpressed EGFR

Previous our study showed that 1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-3-carboxamide analogs had more potent anti-cancer activity than that of gefitinib, which is representative EGFR-TKI, in MDA-MB-468 human breast cancer cells expressing abnormally high level of EGFR. Especially, they more strongly inhibited the phosphorylation of Akt being in the EGFR signaling pathway compared with gefitinib. In this study, we compared their anticancer effect between MDA-MB-468 and A431 epidermoid carcinoma cells which is another model having high level of EGFR. Although the tissue origin is different, they showed similar anticancer activity in both EGFR overexpressing cell lines. These results suggest that 1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-3-carboxamide analogs could be promising agent to overcome EGRF overexpressing cancer cells.