Synthesis of the new ring system pyrrolizino[2,3-b]indol-4(5H)-one
Synthesis of the new ring system pyrrolizino[2,3-b]indol-4(5H)-one
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DOI：
10.1016/j.tet.2011.03.060
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发表时间：
2011-05-13
期刊：
影响因子：
2.1
通讯作者：
Cirrincione, Girolamo
中科院分区：
文献类型：
--
作者：
Diana, Patrizia;Stagno, Antonina;Cirrincione, Girolamo
以邻位带有官能化氨基的取代苯并腈为起始原料，分四步制备了新的环系吡咯利齐诺[2,3-b]吲哚-4(5H)- 1衍生物。未取代的-和二甲氧基吡咯利嗪吲哚酮5a和5b对HL-60（TB）人白血病细胞系表现出适度的活性，而n-甲基化的二甲氧基吡咯利嗪吲哚酮6b对MOLT-4白血病、A549/ATCC、HOP-92和NCI-H460非小细胞肺癌和CAKI-1肾癌细胞系表现出选择性。(C) 2011 Elsevier Ltd.版权所有。
Derivatives of the new ring system pyrrolizino[2,3-b]indol-4(5H)-one were prepared in four steps starting from substituted benzonitriles bearing a functionalized amino group in the adjacent position. The unsubstituted- and the dimethoxy-pyrrolizinoindolones 5a and 5b exhibited modest activity against the HL-60(TB) human leukemia cell line, whereas the N-methylated dimethoxy-pyrrolizinoindolone 6b showed to be selective against MOLT-4 leukemia, A549/ATCC, HOP-92, and NCI-H460 non-small cell lung cancer, and CAKI-1 renal cancer cell lines. (C) 2011 Elsevier Ltd. All rights reserved.