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請使用永久網址來引用或連結此文件:
http://ir.cmu.edu.tw/ir/handle/310903500/28642
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| 題名: | Identification and differentiation of bear bile used in medicinal products in Taiwan |
| 作者: | Lin, DL;Chang, HC;Chang, CP;Chen, CY |
| 貢獻者: | 中國醫藥大學;TAIPEI MED COLL,GRAD INST PHARMACEUT SCI,TAIPEI,TAIWAN;CHINA MED COLL,TAICHUNG,TAIWAN |
| 日期: | 1997 |
| 上傳時間: | 2010-09-24 13:38:58 (UTC+8) |
| 出版者: | AMER SOC TESTING MATERIALS |
| 摘要: | As part of our continuing search for potential anticancer drug candidates:in the 2-aryl-1,8-naphthyridin-4(1H)-one series, we have synthesized two series of 3'-substituted 2-phenyl-1,8-naphthyridin-4(1H)-ones and 2-naphthyl-1,8-naphthyridin-4(1H)-ones. All compounds showed significant cytotoxic effects (log GI(50) < -4.0; log molar drug concentration required to cause 50% growth inhibition) against a variety of human tumor cell lines of the National Cancer Institute's in vitro screen, including cells derived from solid tumors such as non-small cell lung, colon, central nervous system, melanoma, ovarian, prostate, and breast cancers. All 3'-substituted compounds demonstrated strong cytotoxic effects in almost all tumor cell lines. Introduction of an aromatic ring at the 2'- and 3'-positions also generated compounds with potent antitumor activity. Incorporation of an aromatic ring at the 3'- and 4'-positions produced compounds with reduced activity. Interestingly, introduction of a halogen at the 3'-position yielded compounds with different selectivity. for the tumor cell lines tested. All 3'-halogenated compounds (29-36) and compounds 38 and 42-44 were potent inhibitors of tubulin polymerization with activities nearly comparable to those of the potent antimitotic natural products colchicine, podophyllotoxin, and combretastatin A-4. Active agents also inhibited the binding of [H-3]colchicine to tubulin. |
| 關聯: | JOURNAL OF FORENSIC SCIENCES 42(5):817-823 |
| 顯示於類別: | [中國醫藥大學] 期刊論文
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