Sławiński Jarosław, Żołnowska Beata, Orlewska Czesława, Chojnacki Jarosław
Department of Organic Chemistry, Medical University of Gdańsk, Gen. J. Hallera Str. 107, 80416 Gdańsk, Poland.
Department of Chemistry, Gdańsk University of Technology, Narutowicza 11/12, 80233 Gdańsk, Poland.
Monatsh Chem. 2012;143(12):1705-1718. doi: 10.1007/s00706-012-0849-7. Epub 2012 Sep 25.
A series of novel 4-chloro--(4,5-dihydro-5-oxo-1-R-1-1,2,4-triazol-3-yl)-5-methyl-2-(R-methylthio)benzenesulfonamide derivatives have been synthesized as potential anticancer agents. The in vitro antitumor activity of some compounds was evaluated in the US National Cancer Institute (NCI) against the NCI-60 cell line panel. The most prominent compound showed remarkable activity against 13 human tumor cell lines representing lung, colon, CNS, melanoma, ovarian, renal, prostate, and breast at low micromolar GI level in the range of 1.9-3.0 μM.
已合成了一系列新型的4-氯-（4,5-二氢-5-氧代-1-R-1,2,4-三唑-3-基）-5-甲基-2-（R-甲硫基）苯磺酰胺衍生物作为潜在的抗癌剂。在美国国立癌症研究所（NCI）对部分化合物针对NCI-60细胞系进行了体外抗肿瘤活性评估。最突出的化合物在1.9 - 3.0 μM的低微摩尔GI水平下，对代表肺癌、结肠癌、中枢神经系统癌、黑色素瘤、卵巢癌、肾癌、前列腺癌和乳腺癌的13种人类肿瘤细胞系显示出显著活性。
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