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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Synthesis and biological evaluation of novel hydroquinone dimethyl ethers as potential anticancer and antimicrobial agents
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Synthesis and biological evaluation of novel hydroquinone dimethyl ethers as potential anticancer and antimicrobial agents

机译：新型对苯二酚二甲醚类化合物的合成及生物学评价

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摘要

The synthesis of two novel series of quinol dimethyl ethers linked to either various functionalities or to some biologically active nitrogenous heterocycles is described. Nine of the newly synthesized quinol dimethyl ethers 5a, b, 9b, 10a, d, 12a, b, and 13a, b were selected by the NCI and were tested initially at a single high dose (10 muM) in the full NCI 60 cell panel. Four of the screened quinol dimethyl ethers bearing unsubstituted phenylhyd-razone 5a, 4-chlorophenylhydrazone 5b, 4-chlorophenyl-3-sulfanyl-l,2,4-triazole 9b, as well as 4-chloroanilino-1,3,4-oxadiazole 12b moieties satisfied the threshold anti-tumor screen. 4-Chlorophenylhydrazone 5b showed very promising results and accordingly was chosen for in vivo antitumor screening. Thus, compound 5b of the series could be considered as the potential lead for development of novel anticancer agents. In addition, compounds 5a-c, 6a-c, 9a-c, 10a, b, d, e, g, h, lla-c, 12a-c, and 13a-c were screened for their in vitro antimicrobial activity. Some of the tested compounds exhibited special high activity comparable to the reference ampicillin against Pseudomonas aeruginosa and Escherichia coli.
机译：描述了两个新颖的喹诺尔二甲基醚系列的合成，该新颖的喹诺尔二甲基醚与各种官能团或某些生物活性含氮杂环连接。 NCI选择了九种新合成的喹诺尔二甲醚5a，b，9b，10a，d，12a，b和13a，b，并在整个NCI 60细胞中以单次高剂量（10μM）进行了测试面板。带有未取代的苯基氢-重氮酮5a，4-氯苯基hydr 5b，4-氯苯基-3-硫烷基-1,2,4-三唑9b以及4-氯苯胺基-1,3,4-恶二唑的四种经筛选的喹诺尔二甲醚12b部分满足抗肿瘤筛选的阈值。 4-氯苯基hydr5b显示出非常有希望的结果，因此被选择用于体内抗肿瘤筛选。因此，该系列化合物5b可被视为开发新型抗癌剂的潜在先导。另外，筛选了化合物5a-c，6a-c，9a-c，10a，b，d，e，g，h，11a-c，12a-c和13a-c的体外抗菌活性。一些测试化合物对铜绿假单胞菌和大肠杆菌显示出与参比氨苄西林相当的特殊高活性。

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