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

Synthesis and assay of isoquinoline derivatives as HIV-1 Tat-TAR interaction inhibitors
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DOI:
10.1016/j.bmcl.2005.01.068
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发表时间:
2005-09-01
影响因子:
2.7
通讯作者:
Yang, M
Yang, M
中科院分区:
医学4区
文献类型:
--
作者:
He, MZ;Yuan, DK;Yang, M

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以HIV-1 TAR元件为靶点,合成了4个新的异喹啉衍生物。它们结合TAR RNA和抑制Tat-TAR RNA相互作用的能力通过CE分析、Tat依赖性HIV-1 LTR驱动的CAT测定和SIV诱导的合胞体评价来确定。(c)2005爱思唯尔有限公司保留所有权利。
Four new isoquinoline derivatives bearing guanidiniurn 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. (c) 2005 Elsevier Ltd. All rights reserved.