Your browser doesn't support javascript.
loading
Synthesis of amino acid derivatives of 5-alkoxy-3,4-dihalo-2(5H)-furanones and their preliminary bioactivity investigation as linkers.
Luo, Shi-He; Yang, Kai; Lin, Jian-Yun; Gao, Juan-Juan; Wu, Xin-Yan; Wang, Zhao-Yang.
Afiliação
  • Luo SH; School of Chemistry and Environment, South China Normal University, Key Laboratory of Theoretical Chemistry of Environment, Ministry of Education, Guangzhou Key Laboratory of Analytical Chemistry for Biomedicine, Guangzhou 510006, P. R. China. wangzy@scnu.edu.cn and School of Chemistry and Chemical
  • Yang K; School of Chemistry and Environment, South China Normal University, Key Laboratory of Theoretical Chemistry of Environment, Ministry of Education, Guangzhou Key Laboratory of Analytical Chemistry for Biomedicine, Guangzhou 510006, P. R. China. wangzy@scnu.edu.cn and College of Pharmacy, Gannan Medic
  • Lin JY; School of Chemistry and Environment, South China Normal University, Key Laboratory of Theoretical Chemistry of Environment, Ministry of Education, Guangzhou Key Laboratory of Analytical Chemistry for Biomedicine, Guangzhou 510006, P. R. China. wangzy@scnu.edu.cn.
  • Gao JJ; College of Sports and Rehabilitation, Gannan Medical University, Ganzhou, Jiangxi province 341000, P. R. China.
  • Wu XY; School of Chemistry and Environment, South China Normal University, Key Laboratory of Theoretical Chemistry of Environment, Ministry of Education, Guangzhou Key Laboratory of Analytical Chemistry for Biomedicine, Guangzhou 510006, P. R. China. wangzy@scnu.edu.cn.
  • Wang ZY; School of Chemistry and Environment, South China Normal University, Key Laboratory of Theoretical Chemistry of Environment, Ministry of Education, Guangzhou Key Laboratory of Analytical Chemistry for Biomedicine, Guangzhou 510006, P. R. China. wangzy@scnu.edu.cn and School of Chemistry and Chemical
Org Biomol Chem ; 17(20): 5138-5147, 2019 05 28.
Article em En | MEDLINE | ID: mdl-31073571
A series of amino acid derivatives are successfully synthesized via a metal-free C-N coupling reaction of 5-alkoxy-3,4-dihalo-2(5H)-furanones and amino acids. Their structures are well characterized with 1H NMR, 13C NMR, ESI-MS and elemental analysis. As potential linkers of the 2(5H)-furanone unit with other drug moieties containing a hydroxyl or amino group, the effect of amino acids is investigated by comparison with other 2(5H)-furanone compounds by constructing C-O/C-S bonds. The preliminary results of the biological activity assay by the MTT method on a series of cancer cell lines in vitro reveal that the introduction of amino acids basically has no toxic effect. This can lead to these 2(5H)-furanone derivatives being further well-linked with other bioactive moieties with amino or hydroxy groups as expected. Thus, the biological activity assay gives a direction for the design of bioactive 2(5H)-furanones based on these amino acid linkers.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Álcoois / Furanos / Aminoácidos / Antineoplásicos Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Álcoois / Furanos / Aminoácidos / Antineoplásicos Idioma: En Ano de publicação: 2019 Tipo de documento: Article