碳环5'-降“反向”柔性体。设计、合成及初步生物活性
Carbocyclic 5'-nor "reverse" fleximers. Design, synthesis, and preliminary biological activity.
作者信息
Zimmermann Sarah C, Sadler Joshua M, Andrei Graciela, Snoeck Robert, Balzarini Jan, Seley-Radtke Katherine L
机构信息
Department of Chemistry and Biochemistry, University of Maryland, Baltimore County, 1000 Hilltop Circle, Baltimore, MD, 21250, USA.
出版信息
Medchemcomm. 2011 Jul 1;2(7). doi: 10.1039/C1MD00094B.
Abstract
A series of 5'-nor carbocyclic "reverse" flexible nucleosides or "fleximers" have been designed wherein the nucleobase scaffold resembles a "split" purine as well as a substituted pyrimidine. This modification was employed to explore recognition by both purine and pyrimidine metabolizing enzymes. The synthesis of the carbocyclic fleximers and the results of their preliminary biological screening are described herein.
摘要
已设计出一系列5'-去甲碳环“反向”柔性核苷或“柔性异构体”，其中核碱基支架类似“分裂”嘌呤以及取代嘧啶。采用这种修饰来研究嘌呤和嘧啶代谢酶的识别作用。本文描述了碳环柔性异构体的合成及其初步生物学筛选结果。
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