Document Detail

Synthesis and biological evaluation of thiobenzanilides as anticancer agents.
MedLine Citation:
PMID:  18359635     Owner:  NLM     Status:  MEDLINE    
A series of novel thiobenzanilides is described. These compounds have been previously found to show strong biological activity such as antimycotic and antifungal actions. This is the first demonstration on the mechanism of the anticancer effect of thiobenzanilide agents (4a-c) on human melanoma A375 cells. The cytotoxic studies of compounds 4a-c on human melanoma A375 cells indicate thiobenzanilides induced higher cytotoxicity than nitrobenzanilides (3a-c). In addition, DNA flow cytometric analysis shows that 4a-c displays a significant G2/M phase arrest, which progresses to early apoptosis as detected by flow cytometry after double-staining with annexin V and propidium iodide (PI). Because cellular apoptosis is often preceded by the disruption of mitochondrial function, the assessment of mitochondrial function in 4a-c-treated cells is worthy of investigation. Our data revealed that treatment of A375 cells with 4a-c resulted in the loss of mitochondrial membrane potential (DeltaPsi(mt)), a reduction of ATP synthesis, increased reactive oxygen species (ROS) generation, and activation of caspase-3. Thus, we suggest that 4a-c agents are potent inducers of cell apoptosis in A375 cells.
Wan-Ping Hu; Hsin-Su Yu; Yan-Ren Chen; Yi-Min Tsai; Yin-Kai Chen; Chao-Cheng Liao; Long-Sen Chang; Jeh-Jeng Wang
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-03-06
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  16     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2008 May 
Date Detail:
Created Date:  2008-05-12     Completed Date:  2008-08-26     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  5295-302     Citation Subset:  IM    
Faculty of Biotechnology, College of Life Science, Kaohsiung Medical University, Kaohsiung, Taiwan.
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MeSH Terms
Adenosine Triphosphate / metabolism
Anilides / chemical synthesis*,  chemistry,  pharmacology*
Antineoplastic Agents / chemical synthesis*,  chemistry,  pharmacology*
Apoptosis / drug effects*
Benzamides / chemical synthesis*,  chemistry,  pharmacology*
Caspase 3 / drug effects,  metabolism
Cell Cycle / drug effects
Cell Division / drug effects
Cell Proliferation / drug effects
DNA, Mitochondrial / chemistry,  drug effects
Drug Screening Assays, Antitumor
Flow Cytometry / methods
G2 Phase / drug effects
Mitochondrial Membranes / drug effects,  metabolism
Molecular Structure
Reactive Oxygen Species / metabolism
Structure-Activity Relationship
Tumor Cells, Cultured
Reg. No./Substance:
0/Anilides; 0/Antineoplastic Agents; 0/Benzamides; 0/DNA, Mitochondrial; 0/N-(4-bromo-phenyl)-4-nitrothiobenzamide; 0/N-(4-nitrophenyl)-4-nitrothiobenzamide; 0/N-(4-trifluoromethyl-phenyl)-4-nitrothiobenzamide; 0/Reactive Oxygen Species; 56-65-5/Adenosine Triphosphate; 93-98-1/benzanilide; EC 3.4.22.-/Caspase 3

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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