Synthesis and Anti‐HIV Activity of a Series of 6‐Modified 2′, 3′‐Dideoxyguanosine and 2′, 3′‐Didehydro‐2′, 3′‐dideoxyguanosine Analogs. Issue 9 (16th September 2013)

• Record Type: Journal Article
• Authors: Xie, Lujia; Yang, Xiantao; Pan, Delin; Cao, Yingli; Cao, Mou; Lin, Guichun; Guan, Zhu; Guo, Ying; Zhang, Lihe; Yang, Zhenjun
• Is Part Of: Chinese journal of chemistry. Volume 31:Issue 9(2013:Sep.)
• Page Start: 1207
• Page End: 1218
• Publication Date: 2013-09-16
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1002/cjoc.201300440
• Languages: English
• ISSNs: 1001-604X

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>In search of potential 2′, 3′‐dideoxyguanosine (ddG) and 2′, 3′‐didehydro‐2′, 3′‐dideoxyguanosine (D4G) prodrugs, a series of 6‐modified ddG, D4G analogs were synthesized and evaluated for their anti‐HIV activities and cytotoxities in cell‐based assays. All analogs showed low cytotoxicities and some of them displayed benign anti‐HIV activities. The active triphosphate forms <italic>in vivo</italic>, ddGTP and D4TTP, were also synthesized by a novel and facile "one‐pot" method. The recognition of ddGTP and D4TTP by Taq, Therminater DNA polymerase and HIV reverse transcriptase (RT) incorporated in DNA/RNA strands were investigated by a non‐radioactivity method and <italic>K</italic>_m were determined.</p> </abstract>