Back to Search
Start Over
Structure-based design, synthesis and evaluation of novel anthra[1,2-d]imidazole-6,11-dione derivatives as telomerase inhibitors and potential for cancer polypharmacology.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2013 Feb; Vol. 60, pp. 29-41. Date of Electronic Publication: 2012 Nov 29. - Publication Year :
- 2013
-
Abstract
- A series of anthra[1,2-d]imidazole-6,11-dione derivatives were synthesized and evaluated for telomerase inhibition, hTERT expression and suppression of cancer cell growth in vitro. All of the compounds tested, except for compounds 4, 7, 16, 24, 27 and 28 were selected by the NCI screening system. Among them, compounds 16, 39, and 40 repressed hTERT expression without greatly affecting cell growth, suggesting for the selectivity toward hTERT expression. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase and polypharmacological targeting strategy.<br /> (Crown Copyright © 2012. Published by Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Proliferation drug effects
Cell Survival drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Humans
Molecular Structure
Structure-Activity Relationship
Telomerase genetics
Telomerase metabolism
Tumor Cells, Cultured
Antineoplastic Agents pharmacology
Drug Design
Enzyme Inhibitors pharmacology
Telomerase antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 60
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 23279865
- Full Text :
- https://doi.org/10.1016/j.ejmech.2012.11.032