Structure-based design, synthesis and biological evaluation of novel anthra[1,2-d]imidazole-6,11-dione homologues as potential antitumor agents.

Authors :: Chen TC
Yu DS
Huang KF
Fu YC
Lee CC
Chen CL
Huang FC
Hsieh HH
Lin JJ
Huang HS
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2013 Nov; Vol. 69, pp. 278-93. Date of Electronic Publication: 2013 Aug 09.
Publication Year :: 2013
Abstract: By using fragment-based design strategies, a series of 2-thio-substituted anthra[1,2-d]imidazole-6,11-diones were synthesized and evaluated for hTERT repressing activities, cell proliferations, and NCI 60-cell panel assay. Compounds 2, 3, 4, 11, 15 and 35 were selected by the NCI and 3, 4, 11 and 15 represent the GI₅₀, TGI and LC₅₀, respectively. Among them, all were moderate selectivity toward leukemia cancer except for 4 exhibited distinctive selectivity of CNS and renal cancer with 7.403 and 6.475. The overall of test compounds exhibited different cytostatic and cytotoxic activities for further developing potential application as anticancer drugs.<br /> (Crown Copyright © 2013. Published by Elsevier Masson SAS. All rights reserved.)

Subjects :: Anthraquinones chemical synthesis
Anthraquinones chemistry
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Benzimidazoles chemical synthesis
Benzimidazoles chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Cell Survival drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Heterocyclic Compounds, 4 or More Rings chemical synthesis
Heterocyclic Compounds, 4 or More Rings chemistry
Humans
Molecular Structure
Structure-Activity Relationship
Telomerase metabolism
Anthraquinones pharmacology
Antineoplastic Agents pharmacology
Benzimidazoles pharmacology
Drug Design
Enzyme Inhibitors pharmacology
Heterocyclic Compounds, 4 or More Rings pharmacology
Telomerase antagonists & inhibitors

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