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Design, Synthesis, and Anti-Breast Cancer Activity of Novel Fluorinated 7-O-Modified Genistein Derivatives.
Yang, Zhifang; Liu, Yi; Liu, Zhuo; Xu, Qinfang; Liu, Shun; Jiang, Kailin; Shi, Yuanlong; Xu, Wenyu; Yang, Zehua; Mi, Pengbing; Xiang, Yijun; Yao, Xu; Zheng, Xing.
Afiliação
  • Yang Z; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Liu Y; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Liu Z; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Xu Q; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Liu S; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Jiang K; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Shi Y; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Xu W; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Yang Z; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Mi P; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Xiang Y; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Yao X; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
  • Zheng X; Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The Second Affiliated Hospital of University of South Ch
Med Chem ; 19(1): 64-74, 2022.
Article em En | MEDLINE | ID: mdl-35674304
ABSTRACT

BACKGROUND:

Genistein has been limited in clinical application due to its low bioavailability, extremely poor liposolubility, and fast glycosylation rate, though it possesses anti-breast cancer activity. Therefore, the discovery of novel genistein derivatives is an urgency.

OBJECTIVE:

To enhance the anti-breast cancer activity of genistein, a series of novel fluorinated genistein derivatives were synthesized.

METHODS:

Their in vitro antitumor activity was investigated by the MTT assay against three cancer cell lines, via, MDA-MB-231, MCF-7, and MDA-MB-435, respectively.

RESULTS:

Analogs 1d, 2b, and 3b showed remarkable anticancer activities compared to tamoxifen, a clinical anti-breast cancer drug on the market.

CONCLUSION:

The activities against breast cancer of genistein were enhanced by introducing the 7- alkoxyl group and fluorine atom into the B-ring. Therefore, these compounds may be potential candidates for treating breast cancer.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Antineoplásicos Limite: Female / Humans Idioma: En Revista: Med Chem Assunto da revista: QUIMICA Ano de publicação: 2022 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Antineoplásicos Limite: Female / Humans Idioma: En Revista: Med Chem Assunto da revista: QUIMICA Ano de publicação: 2022 Tipo de documento: Article