A new scaffold of topoisomerase I inhibitors: Design, synthesis and biological evaluation

被引：6
|
作者：
Mazza, Alberto [1 ]
Beccalli, Egle M. [1 ]
Contini, Alessandro [1 ]
Garcia-Argaez, Aida Nelly [2 ]
Via, Lisa Dalla [3 ]
Gelmi, Maria Luisa [1 ]
机构：
[1] Univ Milan, DISFARM, Sez Chim Organ A Marchesini, Via Venezian 21, I-20133 Milan, Italy
[2] Fdn Biol & Med Rigeneraz TES Tissue Engn & Signal, Via F Marzolo 13, I-35131 Padua, Italy
[3] Univ Padua, Dipartimento Sci Farmaco, Via F Marzolo 5, I-35131 Padua, Italy
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 124卷
关键词：
Topoisomerase inhibitors; Amination; Pd-catalysis; Pyrroloacridines; Triptamine; Polyheterocyclic systems; <A>ANNULATED CARBAZOLES; DNA TOPOISOMERASES; DRUGS; CAMPTOTHECINS; DERIVATIVES; ANTICANCER; ALKALOIDS; DISCOVERY; ANTITUMOR; POISONS;
D O I：
10.1016/j.ejmech.2016.08.045
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of a new hexacyclic system was realized starting from tryptamines and exploiting as a key step a sequential Pd-catalyzed N-arylation/acylation reaction. Having topoisomerases as biological target and the campthotecins class as benchmark, the new scaffold was decorated with substituents having different polarity and tested as Topoisomerase I inhibitors. (C) 2016 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：326 / 339
页数：14
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