Negishi Cross-Coupling Reaction as a Route to Isocombretastatins

被引：8
作者：
Malysheva, Yulia B. [1 ]
Buchvalova, Svetlana Y. [1 ]
Svirshchevskaya, Elena V. [2 ]
Fokin, Valery V. [3 ]
Fedorov, Alexey Y. [1 ]
机构：
[1] Lobachevsky State Univ Nizhni Novgorod, Dept Organ Chem, Nizhnii Novgorod 603950, Russia
[2] Russian Acad Sci, MM Shemyakin & Yu A Ovchinnikov Inst Bioorgan Che, Moscow 117997, Russia
[3] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
来源：
SYNLETT | 2013年 / 24卷 / 14期
基金：
俄罗斯基础研究基金会;
关键词：
isocombretastatins; antitubulin agents; turbo Grignard reagent; Negishi cross-coupling; cytotoxicity; COMBRETASTATIN A-4 ANALOGS; BIOLOGICAL EVALUATION; 4-ARYLCOUMARIN ANALOGS; ANTINEOPLASTIC AGENTS; SUZUKI-MIYAURA; TUBULIN; MICROTUBULE; HALIDES; 1,1-DIARYLETHYLENES; CHEMISTRY;
D O I：
10.1055/s-0033-1339334
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A series of isocombretastatins A has been synthesized by a new method based on the Negishi cross-coupling reaction in 19-84% yields. Five of the synthesized compounds exhibit high cytotoxic activity in nanomolar concentrations (IC50 = 1-100 nM) towards Jurkat, K562, Colo357, and A549 cell lines.
引用
收藏
页码：1772 / 1776
页数：5
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