IR@PKUHSC  > 北京大学药学院
学科主题药学
Study on the synthesis and PKA-I binding activities of 5-alkynyl tubercidin analogues
Zhang, LG; Zhang, YL; Li, XH; Zhang, LH
刊名BIOORGANIC & MEDICINAL CHEMISTRY
2002-04-01
10期:4页:907-912
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]PROTEIN-KINASE-A ; SYNERGISTIC INHIBITION ; ANTITUMOR-ACTIVITY ; CELL-GROWTH ; NUCLEOSIDES ; CANCER ; 8-CHLOROADENOSINE ; DRUGS ; RNA
英文摘要

5-Alkynyl tubercidin analogues were synthesized and their biological activities were evaluated. It was found that protein kinase A could be activated by 5-alkynyl tubercidin (9a) and cAMP-binding ability to PKA-I was selectively inhibited by it. Molecular modeling showed that the interaction of 9a and PKA-I was associated with the existence of hydrophobic alkynyl group, During (he synthesis of tubercidin analogues, a pair of 2′-carbonyl participating abnormal coupling products (11a, 11b) was obtained, the structure was identified by X-ray crystalline diffraction. (C). 2002 Elsevier Science Ltd. All rights reserved.

语种英语
WOS记录号WOS:000174151500009
Citation statistics
Cited Times:13[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/51167
Collection北京大学药学院
作者单位Peking Univ, Sch Pharmaceut Sci, Natl Res Lab Nat & Biometr Drugs, Beijing 100083, Peoples R China
Recommended Citation
GB/T 7714
Zhang, LG,Zhang, YL,Li, XH,et al. Study on the synthesis and PKA-I binding activities of 5-alkynyl tubercidin analogues[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2002,10(4):907-912.
APA Zhang, LG,Zhang, YL,Li, XH,&Zhang, LH.(2002).Study on the synthesis and PKA-I binding activities of 5-alkynyl tubercidin analogues.BIOORGANIC & MEDICINAL CHEMISTRY,10(4),907-912.
MLA Zhang, LG,et al."Study on the synthesis and PKA-I binding activities of 5-alkynyl tubercidin analogues".BIOORGANIC & MEDICINAL CHEMISTRY 10.4(2002):907-912.
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