e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
Aromatic P 1 replacements for the highly potent HIV-1 protease inhibitor CRIXIVAN®
CA Coburn, MB Young, RW Hungate…
Index: Coburn, Craig A.; Young, Mary Beth; Hungate, Randall W.; Isaacs, Richard C.A.; Vacca, Joseph P.; Huff, Joel R. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 16 p. 1937 - 1940
A series of analogs of CRIXIVAN® containing various aromatic P1 ligands were prepared and evaluated for inhibition of the HIV-1 protease enzyme. These new compounds were found to be effective inhibitors at nanomolar concentrations in the in vitro enzyme inhibition assay as well as the whole cell assay.
![(2R,4S)-2-benzyl-1-((3aS,8aR)-2,2-dimethyl-8,8a-dihydro-2H-indeno[1,2-d]oxazol-3(3aH)-yl)-4-hydroxy-5-(2-methoxyphenyl)pentan-1-one Structure](https://image.chemsrc.com/caspic/414/194204-19-8.png)
![(2R,4S)-2-benzyl-4-hydroxy-N-[(2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5-(2-methoxyphenyl)pentanamide Structure](https://image.chemsrc.com/caspic/232/181869-00-1.png)
![N-[N,O-ISOPROPYLIDENE-(2R)-HYDROXY INDAN-(1S)-YL]-(2R)-BENZYL-(4S,5)-EPOXY PENTANAMIDE Structure](https://image.chemsrc.com/caspic/244/158512-24-4.png)