Synthesis and in vitro evaluation of the antitumor potential and chemo-sensitizing activity of fluorinated ecdysteroid derivatives
Open accessAbstract
Efflux pumps, like the ABCB1 transporter, play an important role in the chemo-resistance of various tumors and particularly of cancer stem cells.
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Fluorinated phytoecdysteroid derivatives increased ABCB1 inhibitory effect and caused inhibition of cell proliferation; derivative compound 5 exerted higher chemo-sensitizing activity to doxorubicin than its parental compound.
“Fluorinated PE derivatives increased the ABCB1 inhibitory effect and caused inhibition of cell proliferation. Also, the derivative compound 5 (14,25-difluoro analog) exerted higher chemo-sensitizing activity to doxorubicin as compared to its parental compound174.”
From The Phytochemical, Biological, and Medicinal Attributes of Phytoecdysteroids: An Updated Review (2021) · cites this paper as [174]
Inclusion of certain oxime ether functions can increase the antiproliferative activity of compound 1 by nearly an order of magnitude on MDA-MB-231 and MCF7 cell lines.
“In our previous study, the antiproliferative IC 50 values of compound 1 were 106.1 and 75.1 mM on the MDA-MB-231 and MCF7 cell lines, respectively [21], showing that the inclusion of certain oxime ether functions can increase this activity by nearly an order of magnitude.”
From Nitrogen-containing ecdysteroid derivatives vs. multi-drug resistance in cancer: Preparation and antitumor activity of oximes, oxime ethers and a lactam (2018) · cites this paper as [21]
A difluorinated derivative of 20E 2,3;20,22-diacetonide is a stronger P-gp inhibitor than parental compound 1.
“a difluorinated derivative of 20E 2,3;20,22diacetonide was found to be a stronger P-gp inhibitor than its parental molecule (compound 1)”
From Nitrogen-containing ecdysteroid derivatives vs. multi-drug resistance in cancer: Preparation and antitumor activity of oximes, oxime ethers and a lactam (2018) · cites this paper as [21]
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References 25 · Cited by 13
- Authors
- Csábi, J., Martins, A., Sinka, I., Csorba, A., Molnár, J., Zupkó, I., Tóth, G., Tillekeratne, L. M. V., & Hunyadi, A.
- Affiliations
- University of Szeged (HU)
- Department of Medical Microbiology and Immunobiology
- University of Toledo (US)
- Corresponding author
- Hunyadi, A.
- Venue
- MedChemComm
- Publisher
- Royal Society of Chemistry (RSC)
- Published
- 2016
- Volume
- 7
- Issue
- 12
- Pages
- 2282-2289
- ISSN
- 2040-2503 (ISSN-L)
- 2040-2511
- OpenAlex
- W2526578338
- Cited by
- 13
- References
- 25
- Citations by year
- 2026: 2 · 2023: 1 · 2022: 2 · 2020: 2 · 2019: 1 · 2018: 1 · 2017: 4
- FWCI
- 0.92
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- MedChemComm (publishedVersion, cc-by-nc)
- SZTE Publicatio Repozitórium (University of Szeged) (acceptedVersion, other-oa)
- Repository of the Academy's Library (Library of the Hungarian Academy of Sciences) (acceptedVersion)
- Funders
- European Cooperation in Science and Technology (CM1106, CM1407)
- Topics
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Natural product bioactivities and synthesis
- Keywords
- anticancer activity, chemosensitization, P-glycoprotein, multidrug resistance, cancer stem cells, efflux pumps
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