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HER2 inhibition efficiency of 6-amino-2-methyl-2-phenethyl-2H-benzopyran and feasibility of the 64Cu-labeled benzopyran derivative in cancer diagnosis

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Abstract

A series of benzopyran derivatives were synthesised, and the target product, 6-amino-2-methyl-2-phenethyl-2H-benzopyran (compound 4), was labeled with radioactive 64Cu (64Cu-6). Compound 4 induced significant apoptosis and suppressed cell proliferation of SK-BR-3 by inhibiting overexpression of the HER2 protein. Furthermore, the 64Cu-6 with significant stability and lipophilicity showed high cellular uptake and cytotoxicity in SK-BR-3, suggesting its promise for dual applications, namely as a diagnostic imaging probe in positron emission tomography (PET) and in cancer treatment.

Graphical abstract: HER2 inhibition efficiency of 6-amino-2-methyl-2-phenethyl-2H-benzopyran and feasibility of the 64Cu-labeled benzopyran derivative in cancer diagnosis

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Publication details

The article was received on 03 Jun 2019, accepted on 26 Oct 2019 and first published on 28 Oct 2019


Article type: Paper
DOI: 10.1039/C9NJ02893E
New J. Chem., 2019, Advance Article

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    HER2 inhibition efficiency of 6-amino-2-methyl-2-phenethyl-2H-benzopyran and feasibility of the 64Cu-labeled benzopyran derivative in cancer diagnosis

    S. Jung, J. R. Anusha, S. Park, K. H. Yu, C. J. Raj and B. C. Kim, New J. Chem., 2019, Advance Article , DOI: 10.1039/C9NJ02893E

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