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Synthesis and activities towards resistant cancer cells of sulfone and sulfoxide griseofulvin derivatives

机译:砜和亚砜灰黄霉素衍生物的合成及其对耐药癌细胞的活性

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Griseofulvin, an antifungal drug, has been shown in recent years to have anti-proliferative activities. We report here the synthesis of new analogs of griseofulvin, substituted in 2' by a sulfonyl group or in 3' by a sulfinyl or sulfonyl group. These compounds exhibit good anti-proliferative activities against SCC114 cells, an oral squamous carcinoma cell line showing pronounced centrosome amplification, and unexpected cytotoxic activities on HCC1937 cells, a triple negative breast cancer cell line resistant to microtubule inhibitors. (C) 2015 Elsevier Ltd. All rights reserved.
机译:灰黄霉素,一种抗真菌药物,近年来已显示出具有抗增殖活性。我们在这里报告了新的灰黄霉素的类似物的合成,其在2'中被磺酰基取代或在3'中被亚磺酰基或磺酰基取代。这些化合物对SCC114细胞,口服鳞状上皮癌细胞系表现出明显的中心体扩增表现出良好的抗增殖活性,并对HCC1937细胞(对微管抑制剂具有抗性的三阴性乳腺癌细胞系)具有出乎意料的细胞毒活性。 (C)2015 Elsevier Ltd.保留所有权利。

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