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Tytuł pozycji:

New chromanone derivatives containing thiazoles: Synthesis and antitumor activity evaluation on A549 lung cancer cell line.

Tytuł:
New chromanone derivatives containing thiazoles: Synthesis and antitumor activity evaluation on A549 lung cancer cell line.
Autorzy:
Yurttaş L; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.
Temel HE; Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.
Aksoy MO; Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.
Bülbül EF; Institute of Pharmacy, Martin Luther University of Halle-Wittenberg, Halle/Saale, Germany.
Çiftçi GA; Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.
Źródło:
Drug development research [Drug Dev Res] 2022 Apr; Vol. 83 (2), pp. 470-484. Date of Electronic Publication: 2021 Sep 17.
Typ publikacji:
Journal Article
Język:
English
Imprint Name(s):
Publication: New York Ny : Wiley-Liss
Original Publication: New York : Alan R. Liss, c1981-
MeSH Terms:
Antineoplastic Agents*/pharmacology
Lung Neoplasms*/drug therapy
A549 Cells ; Apoptosis ; Cell Proliferation ; Drug Screening Assays, Antitumor ; Humans ; Molecular Docking Simulation ; Molecular Structure ; Structure-Activity Relationship ; Thiazoles/pharmacology
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Grant Information:
1805S245 Anadolu University Scientific Research Project, Eskisehir, Turkey
Contributed Indexing:
Keywords: apoptosis; chromane; cytotoxicity; molecular docking
Substance Nomenclature:
0 (Antineoplastic Agents)
0 (Thiazoles)
Entry Date(s):
Date Created: 20210917 Date Completed: 20220502 Latest Revision: 20220524
Update Code:
20240105
DOI:
10.1002/ddr.21879
PMID:
34532880
Czasopismo naukowe
Novel 2-[2-(chroman-4-ylidene)hydrazinyl]-4/5-substituted thiazole derivatives (2a-i) were synthesized and investigated for their anticancer activity. Cytotoxic activity on A549 and NIH/3T3 cell lines was determined, most of the compounds exhibited high cytotoxic profile with selectivity. Selected compounds 2b, 2c, 2e, 2g, 2h, and 2i were tested to determine induction of apoptosis, mitochondrial membrane depolarization, and cell cycle arrest. The results showed that the compounds induced apoptosis intrinsically that they triggered loss of mitochondrial potential through increasing the accumulation of cells in G2/M. Besides, intrinsic apoptotic pathway was supported by down-regulation of anti-apoptotic protein Bcl-2 and up-regulation of proapoptotic protein Bax. Molecular docking study for compounds 2b, 2c, and 2g was promoted experimental outcomes.
(© 2021 Wiley Periodicals LLC.)

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