首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >In vivo antitumor, in vitro antibacterial activity and alkylating properties of phosphorohydrazine derivatives of coumarin and chromone.
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In vivo antitumor, in vitro antibacterial activity and alkylating properties of phosphorohydrazine derivatives of coumarin and chromone.

机译:香豆素和色酮的磷酸肼衍生物的体内抗肿瘤,体外抗菌活性和烷基化特性。

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The aim of this research was to examine chemical and biological properties of the products (4a-c/5a-c, 8b-c, 9a-b) of the reaction of methyl chromone-3-carboxylate (2), 3-formyl-4-hydroxycoumarin (3), 3-formylchromone (6) and chromone 3-carbonyl chloride (7) with phosphorus hydrazides (1a-c). For structure and keto-enol tautomerism analyses (1)H, (13)C, (31)P NMR spectroscopy was used. The ring transformation species (4a-c/5a-c) containing the coumarin ring (5a-c) were predominant in the solution. The chromone series 8b-c and 9a-b was obtained in reaction of phosphorus hydrazides (1a-c) with 3-formylchromone (6) and chromone-3-carbonyl chloride (7). Alkylating activity of phosphorohydrazides of coumarin and chromone was determined with in vitro Preussmann test (NBP test). Some of the compounds were examined towards antitumor and antibacterial activity. Compounds 4b-c/5b-c and 9a demonstrated in vitro antitumor activity against P388 leukemia. Antineoplastic activity of the compounds 4b/5b and 9a combined with methotrexate was showed using L1210 murine leukemia.
机译:这项研究的目的是检查色原-3-羧酸甲酯(2),3-甲酰基- 4-羟基香豆素(3),3-甲酰基色酮(6)和色酮3-羰基氯(7)与酰肼磷(1a-c)。对于结构和酮-烯醇互变异构分析,使用(1)H,(13)C,(31)P NMR光谱。含有香豆素环(5a-c)的环转化物种(4a-c / 5a-c)占主导地位。酰肼(1a-c)与3-甲酰基色酮(6)和色酮-3-羰基氯(7)反应得到色酮系列8b-c和9a-b。香豆素和色酮的磷酸酰肼的烷基化活性通过体外Preussmann试验(NBP试验)测定。检查了一些化合物的抗肿瘤和抗菌活性。化合物4b-c / 5b-c和9a表现出对P388白血病的体外抗肿瘤活性。使用L1210鼠白血病显示了化合物4b / 5b和9a与甲氨蝶呤的抗肿瘤活性。

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