Skip NavigationSkip to Content
Return Return to Search Results

Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones

  1. Author:
    Zhao, X. Z.
    Maddali, K.
    Vu, B. C.
    March, C.
    Hughes, S. H.
    Pommier, Y.
    Burke, T. R.

  2. Author Address

    Zhao, Xue Zhi, Burke, Terrence R., Jr.] NCI, Med Chem Lab, Ctr Canc Res, NIH, Frederick, MD 21702 USA. [Maddali, Kasthuraiah, Marchand, Christophe, Pommier, Yves] NCI, Mol Pharmacol Lab, Ctr Canc Res, NIH, Bethesda, MD 20892 USA. [Vu, B. Christie, Hughes, Stephen H.] NCI, HIV Drug Resistance Program, Ctr Canc Res, NIH, Frederick, MD 21702 USA.
    1. Year: 2009
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 19
    2. 10
    3. Pages: 2714-2717
  4. Type of Article: Article
  1. Abstract:

    Using 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one and 4,5-dihydroxy-1H-isoindole-1,3(2H)-dione based HIV-1 integrase inhibitors as display platforms, we undertook a thorough examination of the effects of modifying the halogen substituents on a key benzyl ring that is hypothesized to bind in a hydrophobic pocket of the integrase. DNA complex. Data from this study suggest that in general dihalo-substituted analogues have higher potency than monohalo-substituted compounds, but that further addition of halogens is not beneficial. Published by Elsevier Ltd.

    See More

  1. Keywords:

External Sources

  1. View Full Text
  2. DOI: 10.1016/j.bmcl.2009.03.122
  3. PMID: 19364649

Library Notes

  1. No notes added.
NCI at Frederick

You are leaving a government website.

This external link provides additional information that is consistent with the intended purpose of this site. The government cannot attest to the accuracy of a non-federal site.

Linking to a non-federal site does not constitute an endorsement by this institution or any of its employees of the sponsors or the information and products presented on the site. You will be subject to the destination site's privacy policy when you follow the link.

ContinueCancel