Synthesis and in vitro antiproliferative activity of new 1,3,4-oxadiazole derivatives possessing sulfonamide moiety
Synthesis and in vitro antiproliferative activity of new 1,3,4-oxadiazole derivatives possessing sulfonamide moiety
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DOI：
10.1016/j.ejmech.2014.11.011
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发表时间：
2015-01-27
影响因子：
6.7
通讯作者：
Oh, Chang-Hyun
中科院分区：
文献类型：
--
作者：
El-Din, Mahmoud M. Gamal;El-Gamal, Mohammed I.;Oh, Chang-Hyun
描述了一系列具有磺酰胺部分的新型 1,3,4-恶二唑衍生物的合成。测试了它们对九种不同癌症类型的 NCI-58 人类癌细胞系的体外抗增殖活性。具有对甲氧基苯磺酰胺基部分的化合物 1k 在 10 μM 浓度下在 58 细胞系组中显示出最高的平均％抑制值。它对不同癌症类型的许多细胞系表现出广谱抗增殖活性。例如，化合物1k在10μM时可抑制T-47D乳腺癌细胞系的生长90.47%。在相同的测试浓度下，它可抑制SR白血病、SK-MEL-5黑色素瘤和MDA-MB-468乳腺癌细胞系的生长80%以上。化合物 1k 对最敏感的细胞系表现出优于 Paditaxel 和 Gefitinib 的活性。 (C) 2014 年 Elsevier Masson SAS。版权所有。
Synthesis of a new series of 1,3,4-oxadiazole derivatives possessing sulfonamide moiety is described. Their in vitro antiproliferative activities against NCI-58 human cancer cell lines of nine different cancer types were tested. Compound 1k with p-methoxybenzenesulfonamido moiety showed the highest mean %inhibition value over the 58 cell line panel at 10 mu M concentration. It showed broad-spectrum antiproliferative activity over many cell lines of different cancer types. For instance, compound 1k inhibited the growth of T-47D breast cancer cell line by 90.47% at 10 mu M. And it inhibited growth of SR leukemia, SK-MEL-5 melanoma, and MDA-MB-468 breast cancer cell lines by more than 80% at the same test concentration. Compound 1k showed superior activity than Paditaxel and Gefitinib against the most sensitive cell lines. (C) 2014 Elsevier Masson SAS. All rights reserved.