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Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors (II)

Hohlfeld, Konrad ; Wegner, Joerg Kurt ; Kesteleyn, Bart ; Linclau, Bruno and Unge, Johan LU (2015) In Journal of Medicinal Chemistry 58(9). p.4029-4038
Abstract
A series of darunavir analogues featuring a substituted bis-THF ring as P2 ligand have been synthesized and evaluated. Very high affinity protease inhibitors (PIs) with an interesting activity on wild-type HIV and a panel of multi-PI resistant HIV-1 mutants containing clinically observed, primary mutations were identified using a cell-based assay. Crystal structure analysis was conducted on a number of PI analogues in complex with HIV-1 protease.
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author
; ; ; and
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Journal of Medicinal Chemistry
volume
58
issue
9
pages
4029 - 4038
publisher
The American Chemical Society (ACS)
external identifiers
  • wos:000354911200027
  • scopus:84929379559
  • pmid:25897791
ISSN
1520-4804
DOI
10.1021/acs.jmedchem.5b00358
language
English
LU publication?
yes
id
3dc8767c-f356-41a8-8dda-4c20af77ca49 (old id 7411700)
date added to LUP
2016-04-01 10:52:17
date last changed
2022-03-20 00:48:06
@article{3dc8767c-f356-41a8-8dda-4c20af77ca49,
  abstract     = {{A series of darunavir analogues featuring a substituted bis-THF ring as P2 ligand have been synthesized and evaluated. Very high affinity protease inhibitors (PIs) with an interesting activity on wild-type HIV and a panel of multi-PI resistant HIV-1 mutants containing clinically observed, primary mutations were identified using a cell-based assay. Crystal structure analysis was conducted on a number of PI analogues in complex with HIV-1 protease.}},
  author       = {{Hohlfeld, Konrad and Wegner, Joerg Kurt and Kesteleyn, Bart and Linclau, Bruno and Unge, Johan}},
  issn         = {{1520-4804}},
  language     = {{eng}},
  number       = {{9}},
  pages        = {{4029--4038}},
  publisher    = {{The American Chemical Society (ACS)}},
  series       = {{Journal of Medicinal Chemistry}},
  title        = {{Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors (II)}},
  url          = {{http://dx.doi.org/10.1021/acs.jmedchem.5b00358}},
  doi          = {{10.1021/acs.jmedchem.5b00358}},
  volume       = {{58}},
  year         = {{2015}},
}