A novel thiazolidine compound induces caspase-9 dependent apoptosis in cancer cells
Date
2012
Authors
Onen-Bayram, F. E.
Durmaz, I.
Scherman, D.
Herscovici, J.
Cetin Atalay, R.
Advisor
Instructor
Source Title
Bioorganic and Medicinal Chemistry
Print ISSN
0968-0896
Electronic ISSN
Publisher
Elsevier
Volume
20
Issue
17
Pages
5094 - 5102
Language
English
Type
Article
Journal Title
Journal ISSN
Volume Title
Abstract
The forward chemogenomics strategy allowed us to identify a potent cytotoxic thiazolidine compound as an apoptosis-inducing agent. Chemical structures were designed around a thiazolidine ring, a structure already noted for its anticancer properties. Initially, we evaluated these novel compounds on liver, breast, colon and endometrial cancer cell lines. The compound 3 (ALC67) showed the strongest cytotoxic activity (IC50 ∼5 μM). Cell cycle analysis with ALC67 on liver cells revealed SubG1/G1 arrest bearing apoptosis. Furthermore we demonstrated that cytotoxicity of this compound was due to the activation of caspase-9 involved apoptotic pathway, which is death receptor independent. © 2012 Elsevier Ltd. All rights reserved.
Course
Other identifiers
Book Title
Keywords
Apoptosis, Cancer, Caspase-9, Cytotoxic, Terminal alkyne, Thiazolidine