| Design, synthesis and antiproliferative activities of novel 5H-pyridazino[4,5-b]indoles |
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| 引用本文： | Rong Dong Li Xin Zhai Yan Fang Zhao Ping Gong. Design, synthesis and antiproliferative activities of novel 5H-pyridazino[4,5-b]indoles[J]. 中国化学快报, 2007, 18(10): 1191-1194. DOI: 10.1016/j.cclet.2007.07.027 |
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| 作者姓名： | Rong Dong Li Xin Zhai Yan Fang Zhao Ping Gong |
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| 作者单位： | Rong Dong Li~(a，b) Xin Zhai~a Yan Fang Zhao~a Ping Gong~(a，*) a School of Pharmaceutical Engineering，Shenyang Pharmaceutical University，Shenyang 110016，China b School of Pharmacy，Hunan University of Traditional Chinese Medicine，Changsha 410208，China |
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| 摘 要： | A novel series of 5H-pyridazino[4,5-b]indoles were designed and synthesized in order to find novel potent anticancer compounds.The structures were confirmed by ~1H NMR and MS.Their antiproliferative activities against two cancer cell lines were tested by the MTT method in vitro.Three of compounds (1e,1g,and 1h) exhibited potent antiproliferative activities,especially compound 1h (with IC_(50) values of 5.2μmol/L and 1.9μmol/L against Bel-7402 and HT-1080,respectively).The preliminary structure-activity relationships of 5H-pyridazino[4,5-b]indole derivatives were discussed.
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| 关 键 词： | 吲哚 派生物 合成方法 化学 |
| 收稿时间： | 2007-04-16 |
| 修稿时间： | 2007-04-16 |
Design, synthesis and antiproliferative activities of novel 5H-pyridazino[4,5-b]indoles |
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| Rong Dong Li,Xin Zhai,Yan Fang Zhao,Ping Gong. Design, synthesis and antiproliferative activities of novel 5H-pyridazino[4,5-b]indoles[J]. Chinese Chemical Letters, 2007, 18(10): 1191-1194. DOI: 10.1016/j.cclet.2007.07.027 |
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| Authors: | Rong Dong Li Xin Zhai Yan Fang Zhao Ping Gong |
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| Affiliation: | 1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China;2. School of Pharmacy, Hunan University of Traditional Chinese Medicine, Changsha 410208, China |
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| Abstract: | A novel series of 5H-pyridazino[4,5-b]indoles were designed and synthesized in order to find novel potent anticancer compounds. The structures were confirmed by 1H NMR and MS. Their antiproliferative activities against two cancer cell lines were tested by the MTT method in vitro. Three of compounds (1e, 1g, and 1h) exhibited potent antiproliferative activities, especially compound 1h (with IC50 values of 5.2 μmol/L and 1.9 μmol/L against Bel-7402 and HT-1080, respectively). The preliminary structure–activity relationships of 5H-pyridazino[4,5-b]indole derivatives were discussed. |
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| Keywords: | 5H-Pyridazino[4,5-b]indole derivatives Synthesis Antipro liferative activities |
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