Document Detail

Tumor-specific cytotoxic activity of 1,2,3,4-tetrahydroisoquinoline derivatives against human oral squamous cell carcinoma cell lines.
MedLine Citation:
PMID:  19661319     Owner:  NLM     Status:  MEDLINE    
The tumor-specific cytotoxicity and the type of cell death induced by thirty-eight newly synthesized tetrahydroisoquinoline derivatives in human oral squamous cell carcinoma cell lines were investigated. 6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)(3,4-dimethoxyphenyl) methanone that has bulky substituents (such as 3,4-dimethoxybenzoyl group) (TQ9) and ethyl 2-benzyloxycarbonyl-1,2,3,4-tetrahydroisoquinoline-1-carboxylate that has ethoxycarbonyl group and benzyloxycarbonyl group (TD13) showed the highest tumor-specific cytotoxicity (TS=12.5 and 5.3, respectively). This supports the importance of molecular size for the cytotoxicity induction. TQ9 induced internulceosomal DNA fragmentation and caspase-3 activation only marginally in HL-60 cells, whereas it enhanced the formation of acidic organelles (stained with acridine orange) without induction of DNA fragmentation or caspase-3 activation in human squamous cell carcinoma cell lines (HSC-2, HSC-4), suggesting the induction of autophagy in the latter cells.
Hajime Hatano; Fumihiro Takekawa; Ken Hashimoto; Mariko Ishihara; Masami Kawase; Chu Qing; Wang Qin-Tao; Hiroshi Sakagami
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Anticancer research     Volume:  29     ISSN:  1791-7530     ISO Abbreviation:  Anticancer Res.     Publication Date:  2009 Aug 
Date Detail:
Created Date:  2009-08-07     Completed Date:  2009-09-30     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8102988     Medline TA:  Anticancer Res     Country:  Greece    
Other Details:
Languages:  eng     Pagination:  3079-86     Citation Subset:  IM    
Division of Pharmacology, Meikai University School of Dentistry, Sakado, Saitama 350-0283, Japan.
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MeSH Terms
Apoptosis / drug effects*
Carcinoma, Squamous Cell / drug therapy*,  pathology*
Caspase 3 / metabolism
Enzyme Activation / drug effects
Mouth Neoplasms / drug therapy*,  pathology*
Organelles / drug effects
Tetrahydroisoquinolines / chemistry*,  pharmacology*
Tumor Cells, Cultured
Reg. No./Substance:
0/Tetrahydroisoquinolines; 91-21-4/1,2,3,4-tetrahydroisoquinoline; EC 3.4.22.-/Caspase 3

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

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