Discovery of benzochromene derivatives first example with dual cytotoxic activity against the resistant cancer cell MCF-7/ADR and inhibitory effect of the P -glycoprotein expression levels Article Swipe
Laila M. Al-Harbi
,
Eman Alharbi
,
Rawda M. Okasha
,
Raafat A. El-Eisawy
,
Mohammed A. A. El-Nassag
,
Hany M. Mohamed
,
Ahmed M. Fouda
,
Ahmed A. Elhenawy
,
Ahmed Mora
,
Ahmed M. El‐Agrody
,
Heba K. Abd El-Mawgoud
·
YOU?
·
· 2023
· Open Access
·
· DOI: https://doi.org/10.1080/14756366.2022.2155814
YOU?
·
· 2023
· Open Access
·
· DOI: https://doi.org/10.1080/14756366.2022.2155814
A series of 1H-benzo[f]chromene moieties (4a-z) were synthesised under Ultrasonic irradiation and confirmed with spectral analyses. Derivative 4i solely possessed an X-ray single crystal. The anti-proliferative efficacy of the desired molecules has been explored against three cancer cells: MCF-7, HCT-116, and HepG-2 with the cytotoxically active derivatives screened against MCF-7/ADR and normal cells HFL-1 and WI-38. Furthermore, compounds 4b-d, 4k, 4n, 4q, and 4w, which possessed good potency against MCF-7/ADR, were tested as permeability glycoprotein (P-glycoprotein [P-gp]) expression inhibitors. The attained data confirmed that 4b-d, 4q, and 4w exhibited strong expression inhibition against the P-gp alongside its cytotoxic effect on MCF-7/ADR. The western blot results and Rho123 accumulation assays showed that compounds 4b-d, 4q, and 4w effectively inhibited the P-gp expression and efflux function. Meanwhile, 4b-d, 4q, and 4w induced apoptosis and accumulation of the treated MCF-7/ADR cells in the G1 phase and 4k and 4n in the S phase of the cell cycle.
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Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1080/14756366.2022.2155814
- OA Status
- gold
- Cited By
- 24
- References
- 82
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W4317548424
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W4317548424Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.1080/14756366.2022.2155814Digital Object Identifier
- Title
-
Discovery of benzochromene derivatives first example with dual cytotoxic activity against the resistant cancer cell MCF-7/ADR and inhibitory effect of the P -glycoprotein expression levelsWork title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2023Year of publication
- Publication date
-
2023-01-20Full publication date if available
- Authors
-
Laila M. Al-Harbi, Eman Alharbi, Rawda M. Okasha, Raafat A. El-Eisawy, Mohammed A. A. El-Nassag, Hany M. Mohamed, Ahmed M. Fouda, Ahmed A. Elhenawy, Ahmed Mora, Ahmed M. El‐Agrody, Heba K. Abd El-MawgoudList of authors in order
- Landing page
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https://doi.org/10.1080/14756366.2022.2155814Publisher 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/10.1080/14756366.2022.2155814Direct OA link when available
- Concepts
-
P-glycoprotein, Cytotoxic T cell, MCF-7, Western blot, Chemistry, Apoptosis, Cytotoxicity, Cancer cell, Cell growth, Molecular biology, In vitro, Pharmacology, Biochemistry, Biology, Multiple drug resistance, Medicine, Cancer, Internal medicine, Gene, Human breast, AntibioticsTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
24Total citation count in OpenAlex
- Citations by year (recent)
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2025: 11, 2024: 6, 2023: 7Per-year citation counts (last 5 years)
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-
82Number of works referenced by this work
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-
10Other works algorithmically related by OpenAlex
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| abstract_inverted_index.active | 45 |
| abstract_inverted_index.assays | 108 |
| abstract_inverted_index.cancer | 36 |
| abstract_inverted_index.cells: | 37 |
| abstract_inverted_index.cycle. | 153 |
| abstract_inverted_index.effect | 98 |
| abstract_inverted_index.efflux | 122 |
| abstract_inverted_index.normal | 51 |
| abstract_inverted_index.series | 1 |
| abstract_inverted_index.showed | 109 |
| abstract_inverted_index.single | 22 |
| abstract_inverted_index.solely | 18 |
| abstract_inverted_index.strong | 89 |
| abstract_inverted_index.tested | 71 |
| abstract_inverted_index.4q</b>, | 113 |
| abstract_inverted_index.against | 34, 48, 68, 92 |
| abstract_inverted_index.desired | 29 |
| abstract_inverted_index.induced | 129 |
| abstract_inverted_index.potency | 67 |
| abstract_inverted_index.results | 104 |
| abstract_inverted_index.treated | 135 |
| abstract_inverted_index.western | 102 |
| abstract_inverted_index.<b>4b-d, | 112 |
| abstract_inverted_index.HCT-116, | 39 |
| abstract_inverted_index.attained | 80 |
| abstract_inverted_index.crystal. | 23 |
| abstract_inverted_index.efficacy | 26 |
| abstract_inverted_index.explored | 33 |
| abstract_inverted_index.moieties | 4 |
| abstract_inverted_index.screened | 47 |
| abstract_inverted_index.spectral | 14 |
| abstract_inverted_index.<b>4i</b> | 17 |
| abstract_inverted_index.<b>4k</b> | 143 |
| abstract_inverted_index.<b>4n</b> | 145 |
| abstract_inverted_index.<b>4w</b> | 87, 115, 128 |
| abstract_inverted_index.MCF-7/ADR | 49, 136 |
| abstract_inverted_index.alongside | 95 |
| abstract_inverted_index.analyses. | 15 |
| abstract_inverted_index.apoptosis | 130 |
| abstract_inverted_index.compounds | 57, 111 |
| abstract_inverted_index.confirmed | 12, 82 |
| abstract_inverted_index.cytotoxic | 97 |
| abstract_inverted_index.exhibited | 88 |
| abstract_inverted_index.function. | 123 |
| abstract_inverted_index.inhibited | 117 |
| abstract_inverted_index.molecules | 30 |
| abstract_inverted_index.possessed | 19, 65 |
| abstract_inverted_index.<b>4k</b>, | 59 |
| abstract_inverted_index.<b>4n</b>, | 60 |
| abstract_inverted_index.<b>4q</b>, | 61, 85, 126 |
| abstract_inverted_index.<b>4w</b>, | 63 |
| abstract_inverted_index.Derivative | 16 |
| abstract_inverted_index.MCF-7/ADR, | 69 |
| abstract_inverted_index.MCF-7/ADR. | 100 |
| abstract_inverted_index.Meanwhile, | 124 |
| abstract_inverted_index.Ultrasonic | 9 |
| abstract_inverted_index.expression | 77, 90, 120 |
| abstract_inverted_index.inhibition | 91 |
| abstract_inverted_index.<i>P-</i>gp | 94 |
| abstract_inverted_index.<i>P</i>-gp | 119 |
| abstract_inverted_index.derivatives | 46 |
| abstract_inverted_index.effectively | 116 |
| abstract_inverted_index.inhibitors. | 78 |
| abstract_inverted_index.irradiation | 10 |
| abstract_inverted_index.synthesised | 7 |
| abstract_inverted_index.<b>4b-d</b>, | 58, 84, 125 |
| abstract_inverted_index.Furthermore, | 56 |
| abstract_inverted_index.accumulation | 107, 132 |
| abstract_inverted_index.glycoprotein | 74 |
| abstract_inverted_index.permeability | 73 |
| abstract_inverted_index.(<b>4a-z</b>) | 5 |
| abstract_inverted_index.cytotoxically | 44 |
| abstract_inverted_index.[<i>P</i>-gp]) | 76 |
| abstract_inverted_index.anti-proliferative | 25 |
| abstract_inverted_index.(<i>P-</i>glycoprotein | 75 |
| abstract_inverted_index.1<i>H</i>-benzo[<i>f</i>]chromene | 3 |
| cited_by_percentile_year.max | 99 |
| cited_by_percentile_year.min | 98 |
| corresponding_author_ids | https://openalex.org/A5032455913 |
| countries_distinct_count | 2 |
| institutions_distinct_count | 11 |
| corresponding_institution_ids | https://openalex.org/I184834183 |
| sustainable_development_goals[0].id | https://metadata.un.org/sdg/3 |
| sustainable_development_goals[0].score | 0.5699999928474426 |
| sustainable_development_goals[0].display_name | Good health and well-being |
| citation_normalized_percentile.value | 0.96997059 |
| citation_normalized_percentile.is_in_top_1_percent | False |
| citation_normalized_percentile.is_in_top_10_percent | True |