Bioorganic & medicinal chemistry

Study on the synthesis and PKA-I binding activities of 5-alkynyl tubercidin analogues

L Zhang, Y Zhang, X Li, L Zhang

Index: Zhang, Liangren; Zhang, Yunlong; Li, Xianghui; Zhang, Lihe Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 4 p. 907 - 912

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Citation Number: 12

Abstract

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 the synthesis of tubercidin analogues, a pair of 2′- ...