Chalcone-benzoxaborole hybrids as novel anticancer agents.

Zhang, Jiong; Yang, Fei; Qiao, Zhitao; Zhu, Mingyan; Zhou, Huchen

Zhang, Jiong; Yang, Fei; Qiao, Zhitao; Zhu, Mingyan; Zhou, Huchen.

Afiliação

Zhang J; State Key Laboratory of Microbial Metabolism, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
Yang F; State Key Laboratory of Microbial Metabolism, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
Qiao Z; State Key Laboratory of Microbial Metabolism, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
Zhu M; State Key Laboratory of Microbial Metabolism, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
Zhou H; State Key Laboratory of Microbial Metabolism, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China; Chemical Biology Division of Shanghai Universities E-Institutes, Key Laboratory of Cell Differentiation and Apoptosis of Chinese Ministry of Education, Shanghai Jiao Tong University Scho

Bioorg Med Chem Lett ; 26(23): 5797-5801, 2016 12 01.

Article em En | MEDLINE | ID: mdl-28327308

ABSTRACT

ABSTRACT

In this study, we report the synthesis of a series of chalcone-benzoxaborole hybrid molecules and the evaluation of their anticancer activity. Their anticancer potency and toxicity were tested on three human cancer cell lines and two normal cell lines. The 4-fluoro compound 15 was found to be the most potent compound with an IC50 value of 1.4µM on SKOV3 cells. The 4-iodo compound 18 and 3-methyloxy-4-amino compound 47 showed good potency on SKOV3 cells while exhibiting low toxicity on normal cells. This work extended the application of benzoxaboroles to the field of anticancer research.

Assuntos

Antineoplásicos/química; Antineoplásicos/farmacologia; Compostos de Boro/química; Compostos de Boro/farmacologia; Chalcona/análogos & derivados; Chalcona/farmacologia; Linhagem Celular Tumoral; Proliferação de Células/efeitos dos fármacos; Descoberta de Drogas; Ensaios de Seleção de Medicamentos Antitumorais; Humanos; Neoplasias/tratamento farmacológico; Relação Estrutura-Atividade

Palavras-chave

Anticancer; Benzoxaborole; Drug discovery; Structureactivity relationship

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Boro / Chalcona / Antineoplásicos Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article País de afiliação: China

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