Chemical Research in Chinese Universities ›› 2009, Vol. 25 ›› Issue (6): 841-845.

• Articles • Previous Articles     Next Articles

Synthesis and Biological Activities of Quinoline Derivatives as HIV-1 Integrase Inhibitors

LUO Zai-gang1, ZENG Cheng-chu1, WANG Fang2, HE Hong-qiu1, WANG Cun-xin1, DU Hong-guang2 and HU Li-ming1*   

  1. 1. College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, P. R. China;
    2. College of Science, Beijing University of Chemical Technology, Beijing 100029, P. R. China
  • Received:2008-11-28 Revised:2009-03-10 Online:2009-11-25 Published:2010-01-25
  • Contact: HU Li-ming. E-mail: huliming@bjut.edu.cn
  • Supported by:

    Supported by the National Basic Research Program of China(No.2009CB930200), Beijing City Education Committee, China (No.KM20061000 5029) and Academic Human Resources Development in Institutions of Higher Learning Under the Jurisdiction?of Beijing Municipality, China.

Abstract:

Based on the structure of the integrase core domain and pharmacophore perception, the authors picked out the hit quinolone derivative 1 as the lead compound via virtual screen in ACD, MDDR, NCI and Chinese Herb three-dimensional database with the aid of DOCK4.0 program and synthesized a series of analogues of compound 1. Their primary anti-HIV properties against integrase reveal that 6-position methyl group on the benzene ring of  quinolone plays a more important role than chlorine, 7-position methyl group or no substituted group. But the    title compounds exhibit little difference when the substituted group was phenyl or thienyl on the pyridine ring of quinoline.

Key words: Quinolone; Integrase; Anti-HIV activity