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Apoptotic Effects of Some Tetrahydronaphthalene Derivatives on K562 Human Chronic Myelogenous Leukemia Cell Line.
- Source :
-
Anti-cancer agents in medicinal chemistry [Anticancer Agents Med Chem] 2018 Feb 07; Vol. 17 (14), pp. 1924-1930. - Publication Year :
- 2018
-
Abstract
- Background: Retinoids which are vitamin A (Retinol) derivatives have been suggested to mediate the inhibition of cancer cell growth and apoptosis. It has been reported that all trans retinoic acid (ATRA) exhibited suppressive effects on different types of leukemia including chronic myelogenous leukemia.<br />Objective: In the present study, we aim to find out the effects of 6 synthetic N-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalene-2-yl)-carboxamide derivatives (compound 6-12) on cell viability and apoptotic pathways in K562 human chronic myelogenous leukemia cell line.<br />Methods: Cell viability and apoptosis were examined by spectrophotometric thiazolyl blue tetrazolium bromide (MTT) and caspase-3 assay, western blot, RT-PCR and flow cytometry.<br />Results: Our results indicated that compound 6 (5-(1,2-Dithiolan-3-yl)-N-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalen-2-yl)pentanamide), 8 (4-(3,4-Dimethoxyphenyl)-N-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalen-2-yl)butanamide) and 11 (E-3-(4-Hydroxy-3-methoxyphenyl)-N-(3,5,5,8,8-pentamethyl- 5,6,7,8-tetrahydronaphthalen-2-yl)acrylamide) exhibited apoptotic effects in K562 human chronic myelogenous leukemia cell line and induced caspase 3, PARP cleavage, Bax/Bcl-2 ratio, Bad and Bim gene expressions.<br />Conclusion: Some retinoid derivatives tested in this study induced apoptosis of K562 cells which suggest that these compounds may serve as potential agents in the treatment of chronic myelogenous leukemia.<br /> (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Proliferation drug effects
Cell Survival drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
K562 Cells
Leukemia, Myelogenous, Chronic, BCR-ABL Positive metabolism
Leukemia, Myelogenous, Chronic, BCR-ABL Positive pathology
Molecular Structure
Structure-Activity Relationship
Tetrahydronaphthalenes chemical synthesis
Tetrahydronaphthalenes chemistry
Tumor Cells, Cultured
Antineoplastic Agents pharmacology
Apoptosis drug effects
Leukemia, Myelogenous, Chronic, BCR-ABL Positive drug therapy
Tetrahydronaphthalenes pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1875-5992
- Volume :
- 17
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Anti-cancer agents in medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 28403785
- Full Text :
- https://doi.org/10.2174/1871521409666170412122811