CCL299, a Benzimidazole Derivative Induces G 1 Phase Arrest and Apoptosis in Cancer Cells

Benzimidazoles are considered potential anticancer candidates. We herein studied the anticancer activity of CCL299, 4-(1H-1,3-benzodiazol-1-yl) benzonitrile. In this in vitro study, we used ATP assays, flow cytometry, western blotting, and caspase-3/7 assays to evaluate the effects of CCL299 on cell...

Full description

Saved in:
Bibliographic Details
Published in:Anticancer research 2021-02, Vol.41 (2), p.699-706
Main Authors: Ohno, Yoshifumi, Yi, Ruirong, Suganami, Akiko, Tamura, Yutaka, Matsumoto, Akio, Matsumoto, Shoji, Saito, Kengo, Shirasawa, Hiroshi
Format: Article
Language:English
Subjects:
A549 Cells
Antineoplastic Agents - pharmacology
Apoptosis - drug effects
Benzimidazoles - pharmacology
Caspase 3 - metabolism
Caspase 7 - metabolism
Cyclin-Dependent Kinase 2 - metabolism
Cyclin-Dependent Kinase Inhibitor p21 - metabolism
Female
G1 Phase Cell Cycle Checkpoints - drug effects
HeLa Cells
Hep G2 Cells
Humans
Neoplasms - drug therapy
Neoplasms - metabolism
Neoplasms - pathology
Signal Transduction
Tumor Suppressor Protein p53 - metabolism
Citations: Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Benzimidazoles are considered potential anticancer candidates. We herein studied the anticancer activity of CCL299, 4-(1H-1,3-benzodiazol-1-yl) benzonitrile. In this in vitro study, we used ATP assays, flow cytometry, western blotting, and caspase-3/7 assays to evaluate the effects of CCL299 on cell proliferation, cell-cycle progression and apoptosis. ATP assays showed that CCL299 inhibited cell growth in the hepatoblastoma cell line HepG2 and the cervical cancer cell line HEp-2, without exhibiting cytotoxic effects on non-cancer cells and TIG-1-20 fibroblasts. Flow cytometry, western blotting, and caspase-3/7 assays revealed that CCL299 induced G -phase cell-cycle arrest followed by apoptosis that was associated with up-regulation of p-p53 (Ser15) and p21 expression and the down-regulation of p-CDK2 (Thr160) expression. CCL299 exhibits cytotoxic activity via apoptosis in a subset of cancer cells, and should be considered as a promising anticancer candidate agent.
ISSN:0250-7005
1791-7530
DOI:10.21873/ANTICANRES.14821