raltegravir-potassium and Colonic-Neoplasms

raltegravir-potassium has been researched along with Colonic-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for raltegravir-potassium and Colonic-Neoplasms

Article	Year
Discovery of 3-acetyl-4-hydroxy-2-pyranone derivatives and their difluoridoborate complexes as a novel class of HIV-1 integrase inhibitors. Bioorganic & medicinal chemistry, 2008, Oct-01, Volume: 16, Issue:19 HIV-1 integrase (IN) has emerged as an important therapeutic target for anti-HIV drug development. Its uniqueness to the virus and its critical role in the viral life cycle makes IN suitable for selective inhibition. The recent approval of Raltegravir (MK-0518) has created a surge in interest and great optimism in the field. In our ongoing IN drug design research, we herein report the discovery of substituted analogs of 3-acetyl-4-hydroxy-2-pyranones and their difluoridoborate complexes as novel IN inhibitors. In many of these compounds, complexation with boron difluoride increased the potency and selectivity of IN inhibition. Compound 9 was most active with an IC(50) value of 9 microM and 3 microM for 3'-processing and strand transfer inhibition, respectively. Topics: Algorithms; Base Sequence; Boron Compounds; Cell Line; Colonic Neoplasms; Fluorides; HIV Integrase Inhibitors; HIV-1; Humans; Inhibitory Concentration 50; Pyrones; Pyrrolidinones; Raltegravir Potassium; Structure-Activity Relationship	2008

Article

Year

Discovery of 3-acetyl-4-hydroxy-2-pyranone derivatives and their difluoridoborate complexes as a novel class of HIV-1 integrase inhibitors.

Bioorganic & medicinal chemistry, 2008, Oct-01, Volume: 16, Issue:19

HIV-1 integrase (IN) has emerged as an important therapeutic target for anti-HIV drug development. Its uniqueness to the virus and its critical role in the viral life cycle makes IN suitable for selective inhibition. The recent approval of Raltegravir (MK-0518) has created a surge in interest and great optimism in the field. In our ongoing IN drug design research, we herein report the discovery of substituted analogs of 3-acetyl-4-hydroxy-2-pyranones and their difluoridoborate complexes as novel IN inhibitors. In many of these compounds, complexation with boron difluoride increased the potency and selectivity of IN inhibition. Compound 9 was most active with an IC(50) value of 9 microM and 3 microM for 3'-processing and strand transfer inhibition, respectively.

Topics: Algorithms; Base Sequence; Boron Compounds; Cell Line; Colonic Neoplasms; Fluorides; HIV Integrase Inhibitors; HIV-1; Humans; Inhibitory Concentration 50; Pyrones; Pyrrolidinones; Raltegravir Potassium; Structure-Activity Relationship

2008