新型苯基支链环丙基核苷的合成及抗hiv活性研究

Ying Wu, Joon Hee Hong
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引用次数: 6

摘要

设计并合成了新型苯基支链环丙基核苷类似物,作为潜在的抗病毒药物。以Zn(Et)2和CH2I2为原料,采用经典的simons - smith反应进行环丙烷化。甲酰基化合物11和12与天然碱基(A、C、T、U)偶联并脱硅得到一系列新的环丙基核苷21-28。合成的化合物对HIV、HSV-1、HSV-2和HCMV等多种病毒的抗病毒和抗肿瘤活性进行了评价。
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Synthesis and anti-HIV activity of novel phenyl branched cyclopropyl nucleosides

Novel phenyl branched cyclopropyl nucleoside analogues were designed and synthesized as potential antiviral agents. Cyclopropanation was performed via classical Simmons–Smith reaction using Zn(Et)2 and CH2I2. Coupling of the mesylates 11 and 12 with natural bases (A,C,T,U) and desilylation afforded a series of novel cyclopropyl nucleosides 2128. The synthesized compounds were evaluated for their antiviral and antitumor activity against various viruses such as HIV, HSV-1, HSV-2 and HCMV.

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