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Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents

  1. Author:
    He, Y. P.
    Long, J.
    Zhang, S. S.
    Li, C.
    Lai, C. C.
    Zhang, C. S.
    Li, D. X.
    Zhang, D. H.
    Wang, H.
    Cai, Q. Q.
    Zheng, Y. T.

  2. Author Address

    [He, Yan-Ping; Zhang, Shui-Shuan; Li, Cong; Zhang, Chun-Sheng; Li, Da-Xiong; Zhang, De-Hua; Wang, Hua; Cai, Qing-Qing] Yunnan Univ, Sch Chem Sci & Technol, Minist Educ, Key Lab Med Chem Nat Resource, Kunming 650091, Peoples R China. [Long, Jin; Zheng, Yong-Tang] Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Lab Mol Immunopharmacol, Kunming 650223, Peoples R China. [Lai, Christopher Cong] NCI, Biol Chem Lab, Ctr Canc Res, Frederick, MD 21702 USA.;He, YP, Yunnan Univ, Sch Chem Sci & Technol, Minist Educ, Key Lab Med Chem Nat Resource, Kunming 650091, Peoples R China.;yphe@ynu.edu.cn zhengyt@mail.kiz.ac.cn
    1. Year: 2011
    2. Date: Jan
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 21
    2. 2
    3. Pages: 694-697
  4. Type of Article: Article
  5. ISSN: 0960-894X
  1. Abstract:

    A novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) combinatory library was synthesized and evaluated with C8166 cells infected by the HIV-1(IIIB) in vitro, using Nevirapine (NVP) and Zidovudine (AZT) as positive control. The anti-HIV screening results revealed that C-6-cyclohexylmethyl substituted pyrimidinones possessed higher selective index than its 6-arylmethyl counterparts. Compounds 1g, 1c, 1e and 1b showed potent anti-HIV activities with EC50 values of 0.012, 0.025, 0.088 and 0.162 nM, respectively. (C) 2010 Elsevier Ltd. All rights reserved.

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External Sources

  1. View Full Text
  2. DOI: 10.1016/j.bmcl.2010.12.003
  3. View record in Web of Science®
  4. WOS: 000285998000015

Library Notes

  1. Fiscal Year: FY2010-2011
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