6-Substituted 1,4-Naphthoquinone Oxime Derivatives (III): Synthesis and Cytotoxic Evaluation
- Autores: Huang G.1, Liu M.1, Meng Q.1, Li S.1
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Afiliações:
- School of Pharmacy
- Edição: Volume 88, Nº 5 (2018)
- Páginas: 1025-1035
- Seção: Article
- URL: https://journals.rcsi.science/1070-3632/article/view/222214
- DOI: https://doi.org/10.1134/S1070363218050316
- ID: 222214
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Resumo
As a continuous study, a set of 23 new 6-substituted 1,4-naphthoquinone oxime derivatives are synthesized and screened for their in vitro cytotoxic activity. Four of those oxime derivatives demonstrate more potent cytotoxic activity towards K562, HCT-15, and HCT-116 cell lines than a reference drug 5-Fu. In particular, compound 21g exhibits the strongest inhibitory activity against K562 cell lines with IC50 values of 1.25 μM. According to flow cytometry data, compound 21g can arrest cell cycle at S phase and induce a strong apoptotic response in K562 cells. The preliminary structure-activity relationship study shows that the nature of substituents in positions 6 and 1' of 1,4-naphthoquinone derivatives significantly affect their cytotoxic activity.
Sobre autores
G. Huang
School of Pharmacy
Autor responsável pela correspondência
Email: guanghuangmedchem@hotmail.com
República Popular da China, Shanghai, 200240
M. Liu
School of Pharmacy
Email: guanghuangmedchem@hotmail.com
República Popular da China, Shanghai, 200240
Q. Meng
School of Pharmacy
Email: guanghuangmedchem@hotmail.com
República Popular da China, Shanghai, 200240
S. Li
School of Pharmacy
Email: guanghuangmedchem@hotmail.com
República Popular da China, Shanghai, 200240