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新型1-(4-(羟基(1-氧代-1,3-二氢-2H-茚-2-亚基)甲基)苯基)-3-苯基脲衍生物的合成与生物学评价

Synthesis and Biological Evaluation of Novel 1-(4-(Hydroxy(1-oxo-1,3-dihydro-2H-inden-2-ylidene)methyl)phenyl)-3-phenylurea Derivatives.

作者信息

Gezegen Hayreddin, Hepokur Ceylan, Tutar Uğur, Ceylan Mustafa

机构信息

Department of Nutrition and Dietetics, Faculty of Health Sciences, Cumhuriyet University, 58140, Sivas, Turkey.

Department of Biochemistry, Faculty of Pharmacy, Cumhuriyet University, 58140, Sivas, Turkey.

出版信息

Chem Biodivers. 2017 Oct;14(10). doi: 10.1002/cbdv.201700223. Epub 2017 Sep 19.

Abstract

A series of novel phenylurea containing 2-benzoylindan-1-one derivatives 3a - 3j were synthesized from the reaction of phenylurea-substituted acetophenones 1a - 1j with phthalaldehyde 2 under mild reaction conditions in good yields. All synthesized compounds were characterized by spectroscopic methods. The obtained compounds (3a - 3j) were evaluated for anticancer activity against HeLa and C6 cell lines. Antiproliferative activity was determined by the BrdU proliferation ELISA assay, 3f and 3g were found to be most active compounds. The compounds were also screened for antimicrobial activity and all compounds showed remarkable activity against used microorganisms.

摘要

通过苯脲取代的苯乙酮1a - 1j与邻苯二甲醛2在温和反应条件下反应,以良好的产率合成了一系列含2 - 苯甲酰基茚满 - 1 - 酮衍生物3a - 3j的新型苯脲。所有合成的化合物均通过光谱方法进行表征。对所得到的化合物(3a - 3j)针对HeLa和C6细胞系进行了抗癌活性评估。通过BrdU增殖ELISA测定法测定抗增殖活性,发现3f和3g是活性最高的化合物。还对这些化合物进行了抗菌活性筛选,所有化合物对所用微生物均表现出显著活性。

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