摘要
原文 | 英語 |
---|---|
頁(從 - 到) | 199-204 |
頁數 | 6 |
期刊 | Oncology Research |
卷 | 13 |
發行號 | 4 |
出版狀態 | 已發佈 - 2002 |
指紋
ASJC Scopus subject areas
- Cancer Research
引用此文
Synthesis and Biological Evaluation of Novel bis-Aziridinylnaphthoquinone Derivatives. / Huang, Sheng Tung; Kuo, Hsien Shou; Lin, Chun-Mao; Tsai, Hsin Da; Peng, Yi Chen; Chen, Chien-Tsu; Lin, Yuh Ling.
於: Oncology Research, 卷 13, 編號 4, 2002, p. 199-204.研究成果: 雜誌貢獻 › 文章
}
TY - JOUR
T1 - Synthesis and Biological Evaluation of Novel bis-Aziridinylnaphthoquinone Derivatives
AU - Huang, Sheng Tung
AU - Kuo, Hsien Shou
AU - Lin, Chun-Mao
AU - Tsai, Hsin Da
AU - Peng, Yi Chen
AU - Chen, Chien-Tsu
AU - Lin, Yuh Ling
PY - 2002
Y1 - 2002
N2 - A series of bis-aziridinylnaphthoquinone derivatives has been prepared. The cytotoxic activities and DNA alkylation abilities of these synthetic bis-aziridinylnaphthoquinone derivatives were investigated. They displayed significant cytotoxicity against human carcinoma cell lines and weak cytotoxic activities against HL60 and skin fibroblast (SF). The bis-aziridinylnaphthoquinone 1a was the most potent agent among those tested, with an LD50 value of 0.57 μM against the BC-M1 cell line. It exhibited the weakest activity against SF and HL60 with LD50 values of 5.67 and 20.1 μM, respectively, and it was able to alkylate DNA after chemical reduction in vitro. The analogues without aziridinyl moiety 2a and 3a lack DNA alkylation abilities.
AB - A series of bis-aziridinylnaphthoquinone derivatives has been prepared. The cytotoxic activities and DNA alkylation abilities of these synthetic bis-aziridinylnaphthoquinone derivatives were investigated. They displayed significant cytotoxicity against human carcinoma cell lines and weak cytotoxic activities against HL60 and skin fibroblast (SF). The bis-aziridinylnaphthoquinone 1a was the most potent agent among those tested, with an LD50 value of 0.57 μM against the BC-M1 cell line. It exhibited the weakest activity against SF and HL60 with LD50 values of 5.67 and 20.1 μM, respectively, and it was able to alkylate DNA after chemical reduction in vitro. The analogues without aziridinyl moiety 2a and 3a lack DNA alkylation abilities.
KW - Bis-Aziridinylnaphthoquinone derivatives
KW - DNA alkylation
KW - Tumor hypoxia
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M3 - Article
C2 - 12659420
AN - SCOPUS:0141889556
VL - 13
SP - 199
EP - 204
JO - Oncology Research
JF - Oncology Research
SN - 0965-0407
IS - 4
ER -