| The synthesis and molecular recognization of the polyamine transporter of hydrazine-modified diamine conjugates |
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| 作者姓名： | Jun Jun Zhou Hao Huang Song Qiang Xie Yu XiaWang Jin Zhao Chao Jie Wang |
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| 作者单位： | a Institute of Natural Products & Medicinal Chemistry, Henan University, Kaifeng 475001, China;b Chemistry Department, Henan University, Kaifeng 475001, China;c Pharmacy College, Henan University, Kaifeng 475001, China |
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| 基金项目： | 国家自然科学基金，河南省自然科学基金 |
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| 摘 要： | A series of four novel hydrazine-modified diamine conjugates （7a-b, 8a-b） were synthesized and evaluated for cytotoxicity against Melanoma B 16, α-difluoromethylornithine （DFMO）-treated B 16, spermidine （SPD）-treated B 16, Mouse leukemia L 1210 and Hela cell lines. Both the DFMO-B 16 and SPD-B 16 experiments indicated that conjugates 7a-b and 8a-b could recognize the polyamine transporter （PAT） and enter the cells in part or in whole via PAT, although they were not as efficient as the reference, 9- anthracenemethyl homospermidine （1）. 2007 Chao Jie Wang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
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| 关 键 词： | 聚胺 合成 生物评价 分子识别 |
| 收稿时间： | 2007-01-19 |
The synthesis and molecular recognization of the polyamine transporter of hydrazine-modified diamine conjugates |
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| Jun Jun Zhou Hao Huang Song Qiang Xie Yu XiaWang Jin Zhao Chao Jie Wang.The synthesis and molecular recognization of the polyamine transporter of hydrazine-modified diamine conjugates[J].Chinese Chemical Letters,2008,19(1):99-101. |
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| Authors: | Jun Jun Zhou Hao Huang Song Qiang Xie Yu Xia Wang Jin Zhao Chao Jie Wang |
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| Institution: | a Institute of Natural Products & Medicinal Chemistry, Henan University, Kaifeng 475001, China;b Chemistry Department, Henan University, Kaifeng 475001, China;c Pharmacy College, Henan University, Kaifeng 475001, China |
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| Abstract: | A series of four novel hydrazine-modified diamine conjugates (7a-b, 8a-b) were synthesized and evaluated for cytotoxicityagainst Melanoma B 16, α-difluoromethylornithine (DFMO)-treated B 16, spermidine (SPD)-treated B 16, Mouse leukemia L 1210and Hela cell lines. Both the DFMO-B 16 and SPD-B 16 experiments indicated that conjugates 7a-b and 8a-b could recognize thepolyamine transporter (PAT) and enter the cells in part or in whole via PAT, although they were not as efficient as the reference, 9-anthracenemethyl homospermidine (1). |
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| Keywords: | Polyamine conjugate Synthesis Bioevaluation |
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