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Anti Human Immunodeficiency Virus Type 1 (HIV-1) Agents 4. Discovery of 5,5 '-(p-Phenylenebisazo)-8-hydroxyquinoline Sulfonates as New HIV-1 Inhibitors in Vitro
Zeng XW1; Huang N2; Xu H*1; Yang WB1; Yang LM2; Qu HA1; Zheng YT*2; orgxuhui@nwsuaf.edu.cn; zhengyt@mail.kiz.ac.cn
2010
发表期刊CHEMICAL & PHARMACEUTICAL BULLETIN
ISSN0009-2363
卷号58期号:7页码:976-979
摘要To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates (4a-j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline p-ethylbenzenesulfonate (4g) and 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline p-chlorobenzenesulfonate (41) showed the more potent anti-HIV-1 activity with 50% effective concentration (EC50) values of 2.59 and 4.01 mu g/ml, and therapeutic index (TI) values of 31.77 and 24.51, respectively.
关键词8-hydroxyquinoline Sulfonate Acquired Immune-deficiency Syndrome Human Immunodeficiency Virus-1 Inhibitor
资助者This work has been supported by the program for New Century Excellent University Talents, State Education Ministry of China (NCET-06-0868), and the Key Project of Chinese Ministry of Educa- tion (No. 107105). We also would like to acknowledge Scientific and Tech- nological Projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185), and the MRC AIDS Research Project and the NIH AIDS Research and Refer- ence Reagent Program for providing cell lines and viruses. ; This work has been supported by the program for New Century Excellent University Talents, State Education Ministry of China (NCET-06-0868), and the Key Project of Chinese Ministry of Educa- tion (No. 107105). We also would like to acknowledge Scientific and Tech- nological Projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185), and the MRC AIDS Research Project and the NIH AIDS Research and Refer- ence Reagent Program for providing cell lines and viruses. ; This work has been supported by the program for New Century Excellent University Talents, State Education Ministry of China (NCET-06-0868), and the Key Project of Chinese Ministry of Educa- tion (No. 107105). We also would like to acknowledge Scientific and Tech- nological Projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185), and the MRC AIDS Research Project and the NIH AIDS Research and Refer- ence Reagent Program for providing cell lines and viruses. ; This work has been supported by the program for New Century Excellent University Talents, State Education Ministry of China (NCET-06-0868), and the Key Project of Chinese Ministry of Educa- tion (No. 107105). We also would like to acknowledge Scientific and Tech- nological Projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185), and the MRC AIDS Research Project and the NIH AIDS Research and Refer- ence Reagent Program for providing cell lines and viruses.
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资助者This work has been supported by the program for New Century Excellent University Talents, State Education Ministry of China (NCET-06-0868), and the Key Project of Chinese Ministry of Educa- tion (No. 107105). We also would like to acknowledge Scientific and Tech- nological Projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185), and the MRC AIDS Research Project and the NIH AIDS Research and Refer- ence Reagent Program for providing cell lines and viruses. ; This work has been supported by the program for New Century Excellent University Talents, State Education Ministry of China (NCET-06-0868), and the Key Project of Chinese Ministry of Educa- tion (No. 107105). We also would like to acknowledge Scientific and Tech- nological Projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185), and the MRC AIDS Research Project and the NIH AIDS Research and Refer- ence Reagent Program for providing cell lines and viruses. ; This work has been supported by the program for New Century Excellent University Talents, State Education Ministry of China (NCET-06-0868), and the Key Project of Chinese Ministry of Educa- tion (No. 107105). We also would like to acknowledge Scientific and Tech- nological Projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185), and the MRC AIDS Research Project and the NIH AIDS Research and Refer- ence Reagent Program for providing cell lines and viruses. ; This work has been supported by the program for New Century Excellent University Talents, State Education Ministry of China (NCET-06-0868), and the Key Project of Chinese Ministry of Educa- tion (No. 107105). We also would like to acknowledge Scientific and Tech- nological Projects of China (2009ZX09501-029, 2008ZX10005-005) and Yunnan (2007BC006), 863 Program (2006AA020602), 973 Program (2009CB522306), the CAS (KSCX1-YW-R-24, KSCX2-YW-R-185), and the MRC AIDS Research Project and the NIH AIDS Research and Refer- ence Reagent Program for providing cell lines and viruses.
文献类型期刊论文
条目标识符http://ir.kiz.ac.cn/handle/152453/4689
专题科研部门_分子免疫药理学(郑永唐)
科研部门_动物模型与人类重大疾病机理重点实验室
通讯作者orgxuhui@nwsuaf.edu.cn; zhengyt@mail.kiz.ac.cn
作者单位1.Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University; Yangling 712100, China
2.Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences; Kunming 650223, China
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Zeng XW,Huang N,Xu H*,et al. Anti Human Immunodeficiency Virus Type 1 (HIV-1) Agents 4. Discovery of 5,5 '-(p-Phenylenebisazo)-8-hydroxyquinoline Sulfonates as New HIV-1 Inhibitors in Vitro[J]. CHEMICAL & PHARMACEUTICAL BULLETIN,2010,58(7):976-979.
APA Zeng XW.,Huang N.,Xu H*.,Yang WB.,Yang LM.,...&zhengyt@mail.kiz.ac.cn.(2010).Anti Human Immunodeficiency Virus Type 1 (HIV-1) Agents 4. Discovery of 5,5 '-(p-Phenylenebisazo)-8-hydroxyquinoline Sulfonates as New HIV-1 Inhibitors in Vitro.CHEMICAL & PHARMACEUTICAL BULLETIN,58(7),976-979.
MLA Zeng XW,et al."Anti Human Immunodeficiency Virus Type 1 (HIV-1) Agents 4. Discovery of 5,5 '-(p-Phenylenebisazo)-8-hydroxyquinoline Sulfonates as New HIV-1 Inhibitors in Vitro".CHEMICAL & PHARMACEUTICAL BULLETIN 58.7(2010):976-979.
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