Synthesis and assay of isoquinoline derivatives as HIV-1 Tat–TAR interaction inhibitors

M He, D Yuan, W Lin, R Pang, X Yu, M Yang

Index: He, Meizi; Yuan, Dekai; Lin, Wei; Pang, Ruifang; Yu, Xiaolin; Yang, Ming Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 17 p. 3978 - 3981

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Citation Number: 25

Abstract

Four new isoquinoline derivatives bearing guanidinium group or amino group-terminated side chain were synthesized to target the HIV-1 TAR element. Their abilities to bind TAR RNA and inhibit Tat–TAR RNA interaction were determined by CE analysis, a Tat- dependent HIV-1 LTR-driven CAT assay and SIV-induced syncytium evaluation.