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Browsing by Author "Boobalan, Ramalingam"

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    Synthesis and biological assay of erlotinib analogues and BSA-conjugated erlotinib analogue
    (2017-04-15)
    Boobalan, Ramalingam
    ;
    Liu, Kuang-Kai
    ;
    Chao, Jui-I.
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    Chen, Chinpiao
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    生物科技學系
    A series of erlotinib analogues that have structural modification at 6,7-alkoxyl positions is efficiently synthesized. The in vitro anti-tumor activity of synthesized compounds is studied in two non-small cell lung cancer (NSCLC) cell lines (A549 and H1975). Among the synthesized compounds, the iodo compound 6 (ETN-6) exhibits higher anti-cancer activity compared to erlotinib. An efficient method is developed for the conjugation of erlotinib analogue-4, alcohol compound, with protein, bovine serum albumin (BSA), via succinic acid linker. The in vitro anti-tumor activity of the protein attached erlotinib analogue, 8 (ETN-4-Suc-BSA), showed stronger inhibitory activity in both A549 and H1975 NSCLC cell lines. (C) 2017 Elsevier Ltd. All rights reserved.