首页> 外文期刊>Monatshefte fur Chemie >Synthesis and molecular structure of novel 2-(alkylthio)-4-chloro-N-(4,5-dihydro-5-oxo-lH-l,2,4-triazol-3-yl)-5-methylbenzene-sulfonamides with potential anticancer activity
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Synthesis and molecular structure of novel 2-(alkylthio)-4-chloro-N-(4,5-dihydro-5-oxo-lH-l,2,4-triazol-3-yl)-5-methylbenzene-sulfonamides with potential anticancer activity

机译:新型2-(烷硫基)-4-氯-N-(4,5-二氢-5-氧代-1H-1,2,4-三唑-3-基)-5-甲基苯磺酰胺的合成及分子结构潜在的抗癌活性

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摘要

A series of novel 4-chloro-N-(4,5-dihydro-5-oxo-1-R~2-1H-1,2,4-triazol-3-yl)-5-methyl-2-(R~1-methylthio)ben-zenesulfonamide 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_(50) level in the range of 1.9-3.0 礛.
机译:一系列新颖的4-氯-N-(4,5-二氢-5-氧代-1-R〜2-1H-1,2,4-三唑-3-基)-5-甲基-2-(R已经合成了〜1-甲硫基)苯-泽磺酰胺衍生物作为潜在的抗癌药。在美国国家癌症研究所(NCI)中评估了某些化合物对NCI-60细胞系的体外抗肿瘤活性。最显着的化合物在1.9-3.0 low的低微摩尔GI_(50)水平下对13种人类肿瘤细胞系表现出显着活性,这些细胞系分别代表肺,结肠,中枢神经系统,黑色素瘤,卵巢,肾,前列腺和乳房。

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