Abstract

Abstract

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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Details

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 levels
Author
Al-Harbi, Laila M 1 ; Al-Harbi, Eman A 2 ; Okasha, Rawda M 2 ; El-Eisawy, R A 3 ; El-Nassag, Mohammed A A 4 ; Mohamed, Hany M 5 ; Fouda, Ahmed M 6 ; Elhenawy, Ahmed A 7 ; Mora, Ahmed 4 ; El-Agrody, Ahmed M 4 ; El-Mawgoud, Heba K A 8 

1  Chemistry Department, Faculty of Science, King Abdul-Aziz University , Jeddah , Saudi Arabia 
2  Chemistry Department, Faculty of Science, Taibah University , Medina , Saudi Arabia 
3  Chemistry Department, Faculty of Science, Al-Azhar University , Cairo , Egypt, Chemistry Department, Faculty of Science and Art, Al-Baha University , Al-Baha , Saudi Arabia 
4  Chemistry Department, Faculty of Science, Al-Azhar University , Cairo , Egypt 
5  Chemistry Department, Faculty of Science, Al-Azhar University , Cairo , Egypt, Chemistry Department, Faculty of Science, Jazan University , Jazan , Saudi Arabia 
6  Chemistry Department, Faculty of Science, King Khalid University , Abha , Saudi Arabia 
7  Chemistry Department, Faculty of Science, Al-Azhar University , Cairo , Egypt, Chemistry Department, Faculty of Science and Art, AlBaha University , Al Bahah , Saudi Arabia 
8  Chemistry Department, Faculty of Women for Arts, Science, and Education, Ain Shams University , Cairo , Egypt 
Publication year
2023
Publication date
Dec 2023
Publisher
Taylor & Francis Ltd.
ISSN
14756366
e-ISSN
14756374
Source type
Scholarly Journal
Language of publication
English
DOI
https://doi.org/10.1080/14756366.2022.2155814
ProQuest document ID
2917549139
Copyright
© 2023 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.. This work is licensed under the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/ (the "License"). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.