首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and primary cytotoxicity evaluation of new 5-benzylidene-2,4-thiazolidinedione derivatives.
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Synthesis and primary cytotoxicity evaluation of new 5-benzylidene-2,4-thiazolidinedione derivatives.

机译:新的5-亚苄基-2,4-噻唑烷二酮衍生物的合成和初步细胞毒性评估。

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摘要

In the present work, ten novel derivatives (3a-3j) of 5-benzylidene-2,4-thiazolidinediones were synthesized and their structures were determined by analytical and spectral (FTIR, (1)H NMR, (13)C NMR) methods. The newly synthesized compounds were evaluated for their antiproliferative activity at Tata Memorial's Advanced Center for Treatment, Research and Education in Cancer (ACTREC), India, in a panel of 7 cancer cell lines using four concentrations at 10-fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. Though the compounds showed varying degrees of cytotoxicity in the tested cell lines, most marked effect was observed by compound 3e in MCF7 (breast cancer), K562 (leukemia) and GURAV (nasopharyngeal cancer) cell lines with log(10) GI(50) values of -6.7, -6.72 and -6.73 respectively.
机译:在本工作中,合成了十个5-亚苄基-2,4-噻唑烷二酮的新型衍生物(3a-3j),并通过分析和光谱法(FTIR,(1)H NMR,(13)C NMR)确定了其结构。 。在印度Tata Memorial癌症治疗,研究和教育高级中心(ACTREC)的7种癌细胞系中,使用4种浓度的10倍稀释液对新合成的化合物的抗增殖活性进行了评估。 Sulforhodamine B(SRB)蛋白测定用于评估细胞稳定性或生长。尽管这些化合物在测试的细胞系中显示出不同程度的细胞毒性,但化合物3e在具有log(10)GI(50)的MCF7(乳腺癌),K562(白血病)和GURAV(鼻咽癌)细胞系中观察到最明显的作用。值分别为-6.7,-6.72和-6.73。

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