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二(3-噻吩基)甲醇和二(3-噻吩基)甲烷的合成及抗癌活性。

Synthesis and anticancer activity of di(3-thienyl)methanol and di(3-thienyl)methane.

机构信息

Plasma Bioscience Research Center, Kwangwoon University, Seoul 139-701, Korea.

出版信息

Molecules. 2012 Sep 27;17(10):11456-68. doi: 10.3390/molecules171011456.

Abstract

Di(3-thienyl)methanol (2) and di(3-thienyl)methane (3) have been synthesized and screened against the T98G (brain cancer) cell line. Treatment induced cell death (MTT and macro-colony assay), growth inhibition, cytogenetic damage (micronuclei formation), were studied as cellular response parameters. Treatment with the compounds enhanced growth inhibition and cell death in a concentration dependent manner in both T98G and HEK (normal) cell lines. At higher concentrations (>20 µg/mL) the cytotoxic effects of the compounds were highly significant. The effect on clonogenic capacity and micronuclei formation observed after treatment of cells. Amongst the compounds, compound 2 exhibited potent activity against T98G brain cancer cells. Despite potent in vitro activity, both compounds exhibited less cytotoxicity against normal human HEK cells at all effective concentrations.

摘要

已合成并筛选了二(3-噻吩基)甲醇(2)和二(3-噻吩基)甲烷(3),以对抗 T98G(脑癌)细胞系。研究了细胞死亡(MTT 和宏观集落测定)、生长抑制、细胞遗传毒性损伤(微核形成)等细胞反应参数。在 T98G 和 HEK(正常)细胞系中,这些化合物以浓度依赖的方式增强了生长抑制和细胞死亡。在较高浓度(>20μg/mL)下,化合物的细胞毒性作用非常显著。处理细胞后观察到对集落形成能力和微核形成的影响。在这些化合物中,化合物 2 对 T98G 脑癌细胞表现出很强的活性。尽管具有很强的体外活性,但在所有有效浓度下,这两种化合物对正常人类 HEK 细胞的细胞毒性都较小。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35a1/6268370/fd9bd7bb6f33/molecules-17-11456-g008.jpg

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