SAR Study and Molecular Mechanism Investigation of Novel Naphthoquinone-furan-2-cyanoacryloyl Hybrids with Antitumor Activity Article Swipe
YOU?
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· 2022
· Open Access
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· DOI: https://doi.org/10.3390/pharmaceutics14102104
A series of novel naphthoquinone-furan-2-cyanoacryloyl hybrids were designed; they were synthesized and preliminarily evaluated for their anti-proliferative activities in vitro against several cancer cell lines and normal cells. The most potent compound, 5c, inhibited the proliferation of HeLa cells (IC50 value of 3.10 ± 0.02 μM) and colony survival, and it induced apoptosis while having relatively weaker effects on normal cells. Compound 5c also triggered ROS generation and accumulation, thus partially contributing to the observed cell apoptosis. A Western blotting analysis demonstrated that compound 5c inhibited the phosphorylation of STAT3. Furthermore, a biolayer interferometry (BLI) analysis confirmed that compound 5c had a direct effect on STAT3, with a KD value of 13.0 μM. Molecular docking showed that 5c specifically occupied the subpockets in the SH2 domain, thereby blocking the whole transmission signaling process. Overall, this study provides an important structural reference for the development of effective antitumor agents.
Related Topics
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.3390/pharmaceutics14102104
- https://www.mdpi.com/1999-4923/14/10/2104/pdf?version=1664618718
- OA Status
- gold
- Cited By
- 2
- References
- 42
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W4303961738
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W4303961738Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.3390/pharmaceutics14102104Digital Object Identifier
- Title
-
SAR Study and Molecular Mechanism Investigation of Novel Naphthoquinone-furan-2-cyanoacryloyl Hybrids with Antitumor ActivityWork title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2022Year of publication
- Publication date
-
2022-10-01Full publication date if available
- Authors
-
Pingxian Liu, Dongmei Fan, Wenliang Qiao, Xinlian He, Lidan Zhang, Yunhan Jiang, Tao YangList of authors in order
- Landing page
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https://doi.org/10.3390/pharmaceutics14102104Publisher landing page
- PDF URL
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https://www.mdpi.com/1999-4923/14/10/2104/pdf?version=1664618718Direct link to full text PDF
- Open access
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YesWhether a free full text is available
- OA status
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goldOpen access status per OpenAlex
- OA URL
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https://www.mdpi.com/1999-4923/14/10/2104/pdf?version=1664618718Direct OA link when available
- Concepts
-
HeLa, Apoptosis, Chemistry, In vitro, Cell culture, Naphthoquinone, Cell biology, Phosphorylation, Furan, Blot, STAT3, Cancer research, Molecular biology, Biochemistry, Biology, Genetics, Gene, Organic chemistryTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
2Total citation count in OpenAlex
- Citations by year (recent)
-
2025: 1, 2023: 1Per-year citation counts (last 5 years)
- References (count)
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42Number of works referenced by this work
- Related works (count)
-
10Other works algorithmically related by OpenAlex
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| citation_normalized_percentile.value | 0.53404792 |
| citation_normalized_percentile.is_in_top_1_percent | False |
| citation_normalized_percentile.is_in_top_10_percent | False |