Investigating the effects of two novel 4-MMPB analogs as potent lipoxygenase inhibitors for prostate cancer treatment Article Swipe
Sonia Iranpour
,
Aseel Kamil Mohammed Al-mosawi
,
Ahmad Reza Bahrami
,
Hamid Sadeghian
,
Maryam Moghaddam Matin
·
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.1186/s40709-021-00141-w
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.1186/s40709-021-00141-w
Background Lipoxygenases are one of the critical signaling mediators which can be targeted for human prostate cancer (PC) therapy. In this study, 4-methyl-2-(4-methylpiperazinyl)pyrimido[4,5-b]benzothiazine (4-MMPB) and its two analogs, 4-propyl-2-(4-methylpiperazinyl)pyrimido[4,5-b]benzothiazine (4-PMPB) and 4-ethyl-2-(4-methylpiperazinyl)pyrimido[4,5-b]benzothiazine (4-EMPB), were proposed to have anti-tumor properties in prostate cancer. Methods After synthesizing the compounds, cytotoxic effects of 4-MMPB and its two analogs against PC-3 cancerous and HDF normal cells were investigated by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay and then mechanism of cell death was assessed by flow cytometry. Finally, the anti-tumor effects of the mentioned compounds were investigated in an immunocompromised C57BL/6 mouse model. Results 4-PMPB and 4-EMPB had similar anti-cancer effects on PC-3 cells as compared with 4-MMPB, while they were not effective on normal cells. Moreover, apoptosis and ferroptosis were the main mechanisms of induced cell death in these cancerous cells. Furthermore, in vivo results indicated that both analogs had similar anti-cancer effects as 4-MMPB, leading to delayed tumor growth without any noticeable side effects in weight loss and histological investigations. Conclusion Thus, our results suggest that specific targeting of lipoxygenases via 4-MMPB analogs can be considered as a treatment of choice for PC therapy, although it requires further investigations.
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Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1186/s40709-021-00141-w
- OA Status
- gold
- Cited By
- 13
- References
- 69
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W3159847810
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
-
https://openalex.org/W3159847810Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.1186/s40709-021-00141-wDigital Object Identifier
- Title
-
Investigating the effects of two novel 4-MMPB analogs as potent lipoxygenase inhibitors for prostate cancer treatmentWork title
- Type
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articleOpenAlex work type
- Language
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enPrimary language
- Publication year
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2021Year of publication
- Publication date
-
2021-05-04Full publication date if available
- Authors
-
Sonia Iranpour, Aseel Kamil Mohammed Al-mosawi, Ahmad Reza Bahrami, Hamid Sadeghian, Maryam Moghaddam MatinList of authors in order
- Landing page
-
https://doi.org/10.1186/s40709-021-00141-wPublisher landing page
- Open access
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YesWhether a free full text is available
- OA status
-
goldOpen access status per OpenAlex
- OA URL
-
https://doi.org/10.1186/s40709-021-00141-wDirect OA link when available
- Concepts
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Flow cytometry, Apoptosis, Prostate cancer, Programmed cell death, Cancer cell, Cytotoxic T cell, In vivo, Chemistry, Cancer research, Cancer, MTT assay, Pharmacology, Biochemistry, In vitro, Biology, Medicine, Molecular biology, Internal medicine, BiotechnologyTop concepts (fields/topics) attached by OpenAlex
- Cited by
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13Total citation count in OpenAlex
- Citations by year (recent)
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2025: 1, 2024: 4, 2023: 4, 2022: 3, 2021: 1Per-year citation counts (last 5 years)
- References (count)
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69Number of works referenced by this work
- Related works (count)
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10Other works algorithmically related by OpenAlex
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