Document Detail

Synthesis and biological activities of 2-amino-1-arylidenamino imidazoles as orally active anticancer agents.
MedLine Citation:
PMID:  20170097     Owner:  NLM     Status:  MEDLINE    
2-Amino-1-arylidenaminoimidazoles, a novel class of orally (po) active microtubule-destabilizing anticancer agents, were synthesized. The compounds were designed from a hit compound identified in a drug discovery platform by using cancer cell-based high throughput screening assay. Selective synthesized compounds exerted cell cytotoxicity against human cancer cells. The underlying mechanisms for the anticancer activity were demonstrated as interacting with the tubulins and inhibiting microtubule assembly, leading to proliferation inhibition and apoptosis induction in the human tumor cells. Furthermore, two compounds showed in vivo anticancer activities in both po and intravenously (iv) administered routes and prolonged the life spans of murine leukemic P388 cells-inoculated mice. These new po active antimitotic anticancer agents are to be further examined in preclinical studies and developed for clinical uses.
Wen-Tai Li; Der-Ren Hwang; Jen-Shin Song; Ching-Ping Chen; Jiunn-Jye Chuu; Chih-Bo Hu; Heng-Liang Lin; Chen-Lung Huang; Chiung-Yi Huang; Huan-Yi Tseng; Chu-Chung Lin; Tung-Wei Chen; Chi-Hung Lin; Hsin-Sheng Wang; Chien-Chang Shen; Chung-Ming Chang; Yu-Sheng Chao; Chiung-Tong Chen
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  53     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2010 Mar 
Date Detail:
Created Date:  2010-03-18     Completed Date:  2010-05-04     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2409-17     Citation Subset:  IM    
Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35 Keyan Road, Zhunan, Miaoli 35053, Taiwan, ROC.
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MeSH Terms
Administration, Oral
Antineoplastic Agents / administration & dosage,  pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Cell Survival / drug effects
DNA Fragmentation / drug effects
Dose-Response Relationship, Drug
Imidazoles / chemical synthesis*,  chemistry,  pharmacology*
Inhibitory Concentration 50
Leukemia P388 / drug therapy,  pathology
Mice, Inbred DBA
Mice, Nude
Microtubules / drug effects,  metabolism
Models, Chemical
Molecular Structure
Neoplasms / drug therapy*,  pathology
Structure-Activity Relationship
Tubulin / metabolism
Xenograft Model Antitumor Assays
Reg. No./Substance:
0/Antineoplastic Agents; 0/Imidazoles; 0/Tubulin

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