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新型单吲哚基-4-三氟甲基吡啶和双吲哚基-4-三氟甲基吡啶的合成与抗肿瘤评价

Synthesis and antitumor evaluation of novel monoindolyl-4-trifluoromethylpyridines and bisindolyl-4-trifluoromethylpyridines.

作者信息

Jiang B, Xiong X N, Yang C G

机构信息

Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, People's Republic of China.

出版信息

Bioorg Med Chem Lett. 2001 Feb 26;11(4):475-7. doi: 10.1016/s0960-894x(00)00704-6.

DOI:10.1016/s0960-894x(00)00704-6
PMID:11229751
Abstract

A series of novel monoindolyl-4-trifluoromethylpyridines and bisindolyl-4-trifluoromethylpyridines was designed and synthesized as potential antitumor agents. They were evaluated for preliminary cytotoxic activity against P388 and A-549 cells with IC50 values. 4-Trifluoromethyl-2,6-bis[3'-(N-tosyl-6'-methoxyl-indolyl)] pyridine was identified as the most potent in this series.

摘要

设计并合成了一系列新型单吲哚基-4-三氟甲基吡啶和双吲哚基-4-三氟甲基吡啶作为潜在的抗肿瘤药物。通过IC50值评估了它们对P388和A-549细胞的初步细胞毒性活性。4-三氟甲基-2,6-双[3'-(N-对甲苯磺酰基-6'-甲氧基-吲哚基)]吡啶被确定为该系列中活性最强的化合物。

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