He Meizi, Yuan Dekai, Lin Wei, Pang Ruifang, Yu Xiaolin, Yang Ming
National Research Laboratory of Natural and Biomimertic Drugs, Peking University, Beijing 100083, China.
Bioorg Med Chem Lett. 2005 Sep 1;15(17):3978-81. doi: 10.1016/j.bmcl.2005.01.068.
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.
合成了四种带有胍基或氨基末端侧链的新型异喹啉衍生物，以靶向HIV-1 TAR元件。通过毛细管电泳分析、基于Tat的HIV-1长末端重复序列驱动的氯霉素乙酰转移酶检测以及猴免疫缺陷病毒诱导的合胞体评估，测定了它们与TAR RNA结合以及抑制Tat-TAR RNA相互作用的能力。
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