Improvement of SNAr Reaction Rate by an Electron‐Withdrawing Group in the Crosslinking of DNA Cytosine‐5 Methyltransferase by a Covalent Oligodeoxyribonucleotide Inhibitor,ChemBioChem

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Improvement of SNAr Reaction Rate by an Electron‐Withdrawing Group in the Crosslinking of DNA Cytosine‐5 Methyltransferase by a Covalent Oligodeoxyribonucleotide Inhibitor
ChemBioChem ( IF 2.6 ) Pub Date : 2018-07-16 , DOI: 10.1002/cbic.201800244
Yukiko Kasai ₁ , Kousuke Sato ₂ , Shohei Utsumi ₁ , Satoshi Ichikawa _{1,

3}

Affiliation

First line of attack: Oligodeoxyribonucleotides containing 2‐amino‐3‐cyano‐4‐halopyridine‐C‐nucleosides (d^XP^CN) form a complex with DNA cytosine‐5 methyltransferases (DNMTs) through a nucleophilic aromatic substitution (S_NAr) reaction. The incorporation of the electron‐withdrawing group (EWG) is effective at increasing the reactivity against nucleophiles of DNMTs, while maintaining high target specificity.

中文翻译：

通过共价寡聚脱氧核糖核苷酸抑制剂的DNA胞嘧啶-5甲基转移酶交联中的吸电子基团提高SNAr反应速率。

攻击的第一行：寡脱氧核糖核苷酸含有2-氨基-3-氰基-4- halopyridine- Ç核苷（d ^X P ^CN）通过亲核芳族取代与DNA形成胞嘧啶-5-甲基转移酶（转移酶）的复合物（S _Ñ AR）反应。吸电子基团（EWG）的引入可有效提高对DNMT亲核试剂的反应性，同时保持较高的靶标特异性。

更新日期：2018-07-16

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