N-苯乙基和N-萘甲基异吲哚酮及其类似物作为体外细胞毒性剂。
N-phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agents.
作者信息
Matesic Lidia, Locke Julie M, Bremner John B, Pyne Stephen G, Skropeta Danielle, Ranson Marie, Vine Kara L
机构信息
School of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia.
出版信息
Bioorg Med Chem. 2008 Mar 15;16(6):3118-24. doi: 10.1016/j.bmc.2007.12.026. Epub 2008 Jan 7.
A range of N-phenethyl, N-phenacyl, and N-(1- and 2-naphthylmethyl) derivatives of 5,7-dibromoisatin 2 were prepared by N-alkylation reactions. Their activity against human monocyte-like histiocytic lymphoma (U937), leukemia (Jurkat), and breast carcinoma (MDA-MB-231) cell lines was assessed. The results allowed further development of structure-activity relationships. The compound 5,7-dibromo-N-(1-naphthylmethyl)-1H-indole-2,3-dione 5a was the most potent against U937 cells with an IC(50) value of 0.19 microM.
通过N-烷基化反应制备了一系列5,7-二溴异吲哚酮2的N-苯乙基、N-苯甲酰基以及N-（1-和2-萘甲基）衍生物。评估了它们对人单核细胞样组织细胞淋巴瘤（U937）、白血病（Jurkat）和乳腺癌（MDA-MB-231）细胞系的活性。这些结果有助于进一步研究构效关系。化合物5,7-二溴-N-（1-萘甲基）-1H-吲哚-2,3-二酮5a对U937细胞的活性最强，IC50值为0.19微摩尔。
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