Synthesis and anti-HBV activity of carbocyclic nucleoside hybrids with salient features of entecavir and aristeromycin,RSC Medicinal Chemistry

当前位置： X-MOL 学术 › RSC Med. Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Synthesis and anti-HBV activity of carbocyclic nucleoside hybrids with salient features of entecavir and aristeromycin
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-05-15 , DOI: 10.1039/d0md00059k
Ramakrishnamraju Samunuri _{1,

2,

3,

4,

5} , Masaaki Toyama _{6,

7,

8,

9,

10} , Renuka Sivasankar Pallaka _{4,

5,

11,

12} , Seshubabu Neeladri _{4,

5,

11,

12} , Ashok Kumar Jha _{4,

5,

11,

12} , Masanori Baba _{6,

7,

8,

9,

10} , Chandralata Bal _{1,

2,

3,

4}

Affiliation

Modified carbocyclic nucleosides (4a–g) constituting 7-deazapurine, 4′-methyl, exocyclic double bond and 2′,3′-hydroxy were synthesized. NOE and X-ray studies of 4c confirmed the α-configuration of 4′-methyl. The anti-HBV assay demonstrated 4e (IC₅₀ = 3.4 μM) without notable cytotoxicity (CC₅₀ = 87.5 μM) as a promising lead for future exploration.

中文翻译：

具有恩替卡韦和阿霉素的突出特征的碳环核苷杂种的合成及抗HBV活性

合成了构成7-脱氮嘌呤，4'-甲基，环外双键和2'，3'-羟基的修饰碳环核苷（4a-g）。4c的NOE和X射线研究证实了4'-甲基的α-构型。抗HBV检测证明4e（IC ₅₀ = 3.4μM）没有明显的细胞毒性（CC ₅₀ = 87.5μM），是未来探索的有希望的线索。

更新日期：2020-05-15

点击分享查看原文

点击收藏

阅读更多本刊最新论文