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Synthesis and anticancer activity evaluation of novel azacalix[2]arene[2]pyrimidines.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2018 May 10; Vol. 151, pp. 214-225. Date of Electronic Publication: 2018 Mar 17. - Publication Year :
- 2018
-
Abstract
- A series of novel azacalix[2]arene[2]pyrimidines were synthesized, and evaluated for their antiproliferative activities against A549, MCF7, SH-SY5Y and CNE human cancer cell lines in vitro by using the CCK-8 assay. A number of compounds showed low micromolar antiproliferative activities against MCF7 cell line. Compound 4j, containing a pyrrolidine moiety, exhibited the strongest inhibitory activity with an IC <subscript>50</subscript> value of 0.58 μM. Furthermore, breast cancer cells were used to explore the inhibition mechanism of these azacalix[2]arene[2]pyrimidines. The results suggested these compounds were involved in inducing cell apoptosis via up-regulation of caspase-3 and caspase-9 protein expression, and the cell cycle was arrested at the S phase. Our reports here represent the first studies on the biological activities of azacalix[2]arene[2]pyrimidines.<br /> (Copyright © 2018 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemical synthesis
Apoptosis drug effects
Breast Neoplasms drug therapy
Calixarenes chemical synthesis
Caspase 3 metabolism
Caspase 9 metabolism
Cell Proliferation drug effects
Drug Design
Drug Screening Assays, Antitumor
Female
Humans
MCF-7 Cells
Pyrimidines chemical synthesis
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Calixarenes chemistry
Calixarenes pharmacology
Pyrimidines chemistry
Pyrimidines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 151
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 29614418
- Full Text :
- https://doi.org/10.1016/j.ejmech.2018.02.079