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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
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Journal of Medicinal Chemistry
volume
58
issue
9
pages
4029 - 4038
publisher
American Chemical Society (ACS)
external identifiers
  • wos:000354911200027
  • scopus:84929379559
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
2015-06-26 14:49:01
date last changed
2017-06-18 03:21:57
@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    = {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},
  volume       = {58},
  year         = {2015},
}