An I<sub>2</sub>–DMSO catalytic manifold enabled aromatization for C-ring editing of podophyllotoxone

Yuan, Peng; Liu, Ronghui; Zhu, Hai‐Liang; Liao, Zhi‐Xin; Xiang, Jia‐Chen; Wu, Yan‐Dong

doi:10.1039/d3ob00927k

Org. Biomol. Chem.

2023

DOI: 10.1039/d3ob00927k

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An I₂–DMSO catalytic manifold enabled aromatization for C-ring editing of podophyllotoxone

Peng Yuan¹,

Ronghui Liu²,

Hai‐Liang Zhu³

et al.

Abstract: The precise aromatization of the C-ring of podophyllotoxone to access value-added dehydropodophyllotoxin derivatives conventionally requires using equivalent of unsustainable oxidants and suffurs from inefficiencies. Taking advantage of the hydridic character...

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Isoxazolidine Derivatives Exhibit Selective Antitumor Activity Against Breast Cancer Cells

Eneama,

Salman,

Mousa

2023

acopen

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Breast cancer, a leading cause of cancer-related mortality in women, necessitates effective therapeutic interventions. Heterocyclic compounds, prevalent in FDA-approved pharmaceuticals, play a pivotal role in drug development. This study focuses on isoxazolidine derivatives, a subgroup of nitrogen and oxygen-containing heterocycles, known for their potential in antitumor applications. A series of novel isoxazolidine compounds were synthesized and evaluated for their anticancer efficacy using MTT assays against MCF-7 and HdFn cell lines, alongside normal cells. Structural elucidation employed FT-IR, 13C-NMR, 1H-NMR, and E-I mass spectroscopy. Results revealed compound (IZ3) with an IC50 value of 32.49 µg/ml, demonstrating notable antitumor activity in MCF-7 cells compared to HdFn. Notably, compounds (IZ1 and IZ2) exhibited IC50 values of 64 µg/ml and 128 µg/ml, respectively. These findings underscore the potential of isoxazolidine derivatives as promising candidates for targeted breast cancer therapies, warranting further investigation in preclinical models and clinical trials. Highlight: Novel Isoxazolidine Compounds: Synthesized and Evaluated Selective Antitumor Activity: Demonstrated in MCF-7 Breast Cancer Cells Promising Therapeutic Candidates: Isoxazolidine Derivatives for Targeted Breast Cancer Therapy Keyword: Breast cancer, Isoxazolidine Derivatives, Antitumor Activity, Heterocyclic Compounds, Drug Development

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Isoxazolidine Derivatives Exhibit Selective Antitumor Activity Against Breast Cancer Cells

Eneama,

Salman,

Mousa

2023

acopen

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An I₂–DMSO catalytic manifold enabled aromatization for C-ring editing of podophyllotoxone

Abstract: The precise aromatization of the C-ring of podophyllotoxone to access value-added dehydropodophyllotoxin derivatives conventionally requires using equivalent of unsustainable oxidants and suffurs from inefficiencies. Taking advantage of the hydridic character...

Cited by 1 publication

References 43 publications

Isoxazolidine Derivatives Exhibit Selective Antitumor Activity Against Breast Cancer Cells

Isoxazolidine Derivatives Exhibit Selective Antitumor Activity Against Breast Cancer Cells

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An I2–DMSO catalytic manifold enabled aromatization for C-ring editing of podophyllotoxone

Abstract: The precise aromatization of the C-ring of podophyllotoxone to access value-added dehydropodophyllotoxin derivatives conventionally requires using equivalent of unsustainable oxidants and suffurs from inefficiencies. Taking advantage of the hydridic character...

Cited by 1 publication

References 43 publications

Isoxazolidine Derivatives Exhibit Selective Antitumor Activity Against Breast Cancer Cells

Isoxazolidine Derivatives Exhibit Selective Antitumor Activity Against Breast Cancer Cells

Contact Info

Product

Resources

About

An I₂–DMSO catalytic manifold enabled aromatization for C-ring editing of podophyllotoxone