Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones.

Authors :: Lee CC
Huang KF
Chang DM
Hsu JJ
Huang FC
Shih KN
Chen CL
Chen TC
Chen RH
Lin JJ
Huang HS
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2012 Apr; Vol. 50, pp. 102-12. Date of Electronic Publication: 2012 Feb 01.
Publication Year :: 2012
Abstract: A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.<br /> (Crown Copyright Â© 2012. Published by Elsevier Masson SAS. All rights reserved.)

Subjects :: Alkaline Phosphatase metabolism
Apoptosis drug effects
Humans
Telomerase metabolism
Tumor Cells, Cultured
Anthraquinones chemistry
Cell Proliferation drug effects
Drug Design
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Neoplasms drug therapy
Telomerase antagonists & inhibitors

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