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

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...

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Published inNew journal of chemistry Vol. 43; no. 47; pp. 18657 - 18662
Main Authors Jung, Soonjae, Anusha, J R, Park, Seungil, Yu, Kook Hyun, Raj, C Justin, Kim, Byung Chul
Format Journal Article
LanguageEnglish
Published Cambridge Royal Society of Chemistry 01.01.2019
Subjects
Apoptosis
Cancer
Diagnostic software
Diagnostic systems
Lipophilicity
Positron emission
Tomography
Toxicity
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Summary: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.
ISSN:1144-0546
1369-9261
DOI:10.1039/c9nj02893e