Design and synthesis of photoactivatable coumarin-containing HIV-1 integrase inhibitors

被引:0
|
作者
Zhao, H [1 ]
Neamati, N [1 ]
Pommier, Y [1 ]
Burke, TR [1 ]
机构
[1] NCI,MOL PHARMACOL LAB,DIV BASIC SCI,NIH,BETHESDA,MD 20892
关键词
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Three dimeric coumarin analogues (1-3) were prepared, each containing the photoactivatable benzophenone moiety. These compounds exhibited low micromolar IC50 values against HIV-1 integrase mediated 3'-processing and strand transfer, and may represent useful probes for elucidating enzyme-inhibitor interactions.
引用
收藏
页码:2277 / 2282
页数:6
相关论文
共 50 条
  • [41] Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors
    Sechi, Mario
    Rizzi, Giuseppe
    Bacchi, Alessia
    Carcelli, Mauro
    Rogolino, Dominga
    Pala, Nicolino
    Sanchez, Tino W.
    Taheri, Laleh
    Dayam, Raveendra
    Neamati, Nouri
    BIOORGANIC & MEDICINAL CHEMISTRY, 2009, 17 (07) : 2925 - 2935
  • [42] HIV-1 integrase strand-transfer inhibitors: Design, synthesis and molecular modeling investigation
    De Luca, Laura
    De Grazia, Sara
    Ferro, Stefania
    Gitto, Rosaria
    Christ, Frauke
    Debyser, Zeger
    Chimirri, Alba
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (02) : 756 - 764
  • [43] Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors
    Patel, Manoj
    Naidu, B. Narasimhulu
    Dicker, Ira
    Higley, Helen
    Lin, Zeyu
    Terry, Brian
    Protack, Tricia
    Krystal, Mark
    Jenkins, Susan
    Parker, Dawn
    Panja, Chiradeep
    Rampulla, Richard
    Mathur, Arvind
    Meanwell, Nicholas A.
    Walker, Michael A.
    BIOORGANIC & MEDICINAL CHEMISTRY, 2020, 28 (13)
  • [44] Classification and Design of HIV-1 Integrase Inhibitors Based on Machine Learning
    Zhou, Junlin
    Hao, Juan
    Peng, Lianxin
    Duan, Huaichuan
    Luo, Qing
    Yan, Hailian
    Wan, Hua
    Hu, Yichen
    Liang, Li
    Xie, Zhenjian
    Liu, Wei
    Zhao, Gang
    Hu, Jianping
    COMPUTATIONAL AND MATHEMATICAL METHODS IN MEDICINE, 2021, 2021
  • [45] Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors
    Sechi, Mario
    Azzena, Ugo
    Delussu, Maria Paola
    Dallocchio, Roberto
    Dessi, Alessandro
    Cosseddu, Alessia
    Pala, Nicolino
    Neamati, Nouri
    MOLECULES, 2008, 13 (10): : 2442 - 2461
  • [46] Rational design of 2-pyrrolinones as inhibitors of HIV-1 integrase
    Ma, Kaiqing
    Wang, Penghui
    Fu, Wei
    Wan, Xiaolong
    Zhou, Lu
    Chu, Yong
    Ye, Deyong
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (22) : 6724 - 6727
  • [47] Synthesis and Evaluation of Aryl Quinolines as HIV-1 Integrase Multimerization Inhibitors
    Jentsch, Nicholas G.
    Hart, Alison P.
    Hume, Jared D.
    Sun, Jian
    McNeely, Kaitlin A.
    Lama, Chiyang
    Pigza, Julie A.
    Donahue, Matthew G.
    Kessl, Jacques J.
    ACS MEDICINAL CHEMISTRY LETTERS, 2018, 9 (10): : 1007 - 1012
  • [48] Synthesis and biological evaluation of geminal disulfones as HIV-1 integrase inhibitors
    Meadows, DC
    Mathews, TB
    North, TW
    Hadd, MJ
    Kuo, CL
    Neamati, N
    Gervay-Hague, J
    JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (14) : 4526 - 4534
  • [49] Synthesis and Biological Activities of Quinoline Derivatives as HIV-1 Integrase Inhibitors
    Luo Zai-gang
    Zeng Cheng-chu
    Wang Fang
    He Hong-qiu
    Wang Cun-xin
    Du Hong-guang
    Hu Li-ming
    CHEMICAL RESEARCH IN CHINESE UNIVERSITIES, 2009, 25 (06) : 841 - 845
  • [50] Design and synthesis of dimeric HIV-1 integrase inhibitory peptides
    Krajewski, K
    Long, YQ
    Marchand, C
    Pommier, Y
    Koller, PP
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (19) : 3203 - 3205