Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae
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DOI：
10.1016/j.bmcl.2010.03.066
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发表时间：
2010-05-01
影响因子：
2.7
通讯作者：
Pagliarin, Roberto
中科院分区：
文献类型：
--
作者：
Coccetti, Paola;Montano, Giuseppe;Pagliarin, Roberto
合成了一系列在30位含有不同取代基(OH、F、NO(2)、NH(2)、B(OH)(2))的Z和E类化合物。通过监测它们在酿酒酵母中抑制细胞生长的能力，分析了这些衍生物和Z和E化合物A-1。化合物A-1(2a)、A-4(2b)和化合物2c对酵母菌生长有抑制作用。此外，联合他汀A-4(2b)和化合物2c通过影响主要的S期细胞周期蛋白Clb5蛋白的合成而诱导细胞周期停滞于G1期。G1期的停滞与应激激活的激酶Snf1的激活是一致的。(C)2010爱思唯尔有限公司。保留所有权利。
A series of Z and E combretastatin A-4 analogs bearing different substituents (OH, F, NO(2), NH(2), B(OH)(2)) in the 30 position were synthesized. These derivatives and Z and E combretastatin A-1 were analysed by monitoring their ability to inhibit cell growth in Saccharomyces cerevisiae. Combretastatin A-1 (2a), A-4 (2b) and compound 2c were found to inhibit yeast growth. Moreover, combretatstatin A-4 (2b) and compound 2c induced a G1 arrest by affecting the synthesis of Clb5 protein, the principal S-phase cyclin. The G1 arrest is coincident with the activation of the stress activated kinase Snf1. (C) 2010 Elsevier Ltd. All rights reserved.