Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors (II)
(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.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/7411700
- author
- Hohlfeld, Konrad ; Wegner, Joerg Kurt ; Kesteleyn, Bart ; Linclau, Bruno and Unge, Johan LU
- organization
- publishing date
- 2015
- 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}}, }