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新型吡啶、色烯、噻吩和噻唑衍生物的合成及抗氧化和抗肿瘤活性。

Synthesis and antioxidant and antitumor activity of novel pyridine, chromene, thiophene and thiazole derivatives.

机构信息

Department of Chemistry, Faculty of Science, Mansoura University, Mansoura, Egypt.

出版信息

Arch Pharm (Weinheim). 2012 May;345(5):378-85. doi: 10.1002/ardp.201100335. Epub 2011 Dec 20.

Abstract

2-Tosylacetonitrile (1) when reacted with α,β-unsaturated nitriles 2a-c or a mixture of formaldehyde and 3-amino-2-substituted-pent-2-endinitriles 6a,b yielded pyridine derivatives 3a-c and 9a,b, respectively, while when subjected to react with salicylaldehyde yielded chromene derivatives 4 and 5, subsequently. The behavior of thiocarbamoyl derivative 10 derived from 1 towards some α-halogenated compounds have been investigated as well as its behavior towards elemental sulfur and phenyl isothiocyanate. Newly synthesized compounds were screened for their antioxidant activity, erythrocytes haemolysis and bleomycin-independent DNA damage. Some of the tested compounds exhibited promising activities.

摘要

2-对甲苯磺酰乙腈(1)与α,β-不饱和腈 2a-c 或甲醛和 3-氨基-2-取代戊-2-烯二腈 6a,b 的混合物反应,分别生成吡啶衍生物 3a-c 和 9a,b,随后与水杨醛反应生成色烯衍生物 4 和 5。研究了硫代甲酰胺基衍生物 10 对一些α-卤代化合物的反应性,以及它对元素硫和异硫氰酸苯酯的反应性。对新合成的化合物进行了抗氧化活性、红细胞溶血和博来霉素非依赖性 DNA 损伤的筛选。一些测试的化合物表现出了有希望的活性。

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