Tumor-specific cytotoxic activity of 1,2,3,4-tetrahydroisoquinoline derivatives against human oral squamous cell carcinoma cell lines.

Full Abstract

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.

Author information

Author/s: Hatano, Hajime (H); Takekawa, Fumihiro (F); Hashimoto, Ken (K); Ishihara, Mariko (M); Kawase, Masami (M); Qing, Chu (C); Qin-Tao, Wang (W); Sakagami, Hiroshi (H);

Affiliation: Division of Pharmacology, Meikai University School of Dentistry, Sakado, Saitama 350-0283, Japan.

Journal and publication information

Publication Type: Journal Article; Research Support, Non-U.S. Gov't

Journal: Anticancer research (Anticancer Res), published in Greece. (Language: eng)

Reference: 2009-Aug; vol 29 (issue 8) : pp 3079-86

Dates: Created 2009/08/07; Completed 2009/09/30;

PMID: 19661319, status: MEDLINE (last retrieval date: 9/30/2009, IMS Date: )

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