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Anti-AIDS agents 86. Synthesis and anti-HIV evaluation of 2 ',3 '-seco-3 '-nor DCP and DCK analogues 期刊论文

编号：

14b9ba92-c127-4729-920f-00aec18f0b97
作者：

Chen, Ying(陈瑛)#^[1]Cheng, Ming^[1];Liu, FaQiang^[1];Xia, Peng(夏鹏)*^[1]Qian, Keduo^[2];Yu, Donglei^[2];Xia, Yi^[2];Yang, ZhengYu^[2];Chen, ChinHo^[3];MorrisNatschke, Susan L.^[2];Lee, KuoHsiung^[2,4];
地址：

[1]Fudan Univ, Sch Pharm, Dept Med Chem, Shanghai 201203, Peoples R China;
[2]Univ N Carolina, Nat Prod Res Labs, UNC Eshelman Sch Pharm, Chapel Hill, NC 27599 USA;
[3]Duke Univ, Med Ctr, Durham, NC 27710 USA;
[4]China Med Univ & Hosp, Chinese Med Res & Dev Ctr, Taichung, Taiwan
语种：

English
期刊：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY ISSN：0223-5234 2011 年 46 卷 10 期 (4924 - 4936) ; OCT
收录：
关键词：

2 ',3 '-Seco-3 '-nor-DCPs Anti-HIV activity Structure-activity relationship (SAR)
摘要：

In a continuing study of novel anti-HIV agents with drug-like structures and properties, 30 1'-O-, 1'-S-, 4'-O- and 4'-substituted-2',3'-seco-3'-nor DCP and DCK analogues (8-37) were designed and synthesized. All newly synthesized seco-compounds were screened against HIV-1(NL4-3) and a multiple reverse transcriptase (RT) inhibitor-resistant (RTMDR) strain in the TZM-bl cell line, using seco-DCK (7) and 2-ethyl-DCP (4) as controls. Several compounds (14, 18, 19, 22-24, and 32) exhibited potent anti-HIV activity with EC50 values ranging from 0.93 to 1.93 mu M and therapeutic index (TI) values ranging from 20 to 39. 1'-O-Isopropoxy-2',3'-seco-3'-nor-DCP (12) showed the greatest potency among the newly synthesized compounds with EC50 values of 0.47 and 0.88 mu M, and TI of 96 and 51, respectively, against HIV-1(NL4-3) and RTMDR strains. The seco-compounds exhibited better chemical stability in acidic conditions compared with DCP and DCK compounds. Overall, the results suggested that seco-DCP analogues with simplified structures may be more favorable for development as novel anti-HIV candidates. (C) 2011 Elsevier Masson SAS. All rights reserved.
推荐引用方式
GB/T 7714：

Chen Ying,Cheng Ming,Liu Fa-Qiang, et al. Anti-AIDS agents 86. Synthesis and anti-HIV evaluation of 2 ',3 '-seco-3 '-nor DCP and DCK analogues [J].EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2011,46(10):4924-4936.
APA：

Chen Ying,Cheng Ming,Liu Fa-Qiang,Xia Peng,&Lee Kuo-Hsiung.(2011).Anti-AIDS agents 86. Synthesis and anti-HIV evaluation of 2 ',3 '-seco-3 '-nor DCP and DCK analogues .EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,46(10):4924-4936.
MLA：

Chen Ying, et al. "Anti-AIDS agents 86. Synthesis and anti-HIV evaluation of 2 ',3 '-seco-3 '-nor DCP and DCK analogues" .EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 46,10(2011):4924-4936.

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