頁籤選單縮合
題名 | Synthesis and Structure-Activity Relationship Studies of Cytotoxic Acridin-9-one Derivatives= |
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作者 | 蘇燦隆; 陳靜煌; 李宜臻; Su, Tsann-long; Chen, Ching-huang; Lee, Yi-jen; |
期刊 | 中華藥學雜誌 |
出版日期 | 19990200 |
卷期 | 51:1 1999.02[民88.02] |
頁次 | 頁103-115 |
分類號 | 418.2216 |
語文 | eng |
關鍵詞 | Glyfoline; Acridin-9-one; Cross-resistance; Cancer therapy; |
英文摘要 | Several 1-hydroxy and 1-amino-10- methylacridin-9-one derivatives were synthesized either starting from the condensation of substituted anthranilic acids with 2-bromo-1,4-dimethoxybenzene or from the reaction of diphenyliodonium-2-carboxylate (DPIC) with 2-methoxy- or 2-methyl-4-nitroaniline. These compounds were subjected for evaluation of their inhibitory effects on the cell growth of several human tumor cells in vitro. Of these compounds, 1,6-dihydroxy-4,5-di-methoxy-10-niethylacridin-9-one (9) was more cytotoxic than glyfoline (an antineoplastic acridone alkaloid) against human colon cancer (COLO205) cell growth in vitro, but as potent as glyfoline against human leukemia (MOLT-4), lung carcinoma H23 and H23's MDR cell line resistant to doxorubicin (H23/0.3). 4,10-Dimethyl- 1 -(N,N-dimethylaminoethylamino)acridin-9-one (16b) was also active on the inhibition of C0L0205 and MOLT-4 cell growth in culture. All acridin-9-ones tested were shown to have very little cross-resistance to doxorubicin. This suggests compound 9 and 16b may be useful in drug-combination cancer therapy with other currently available anticancer drugs. |
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