G. N. Krishnamurthy

Learn More
HCV-796 selectively inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. In hepatoma cells containing a genotype 1b HCV replicon, HCV-796 reduced HCV RNA levels by 3 to 4 log(10) HCV copies/mug total RNA (the concentration of the compound that inhibited 50% of the HCV RNA level was 9 nM). Cells bearing replicon variants with reduced(More)
A novel series of inhibitors of cancer cell proliferation, selective against p21 cell cycle checkpoint-disrupted cells vs. cells with intact p21 checkpoint, were identified by high-throughput screening. Optimization of both ends of the lead molecule to improve potency, using parallel synthesis and iterative design, is described. The(More)
New metal complexes of the type [M(nih)(L)](PF(6))(n)·xH(2)O and [M(nih)(2)](PF(6))·xH(2)O (where M=Co(III) or Ni(II), L=1,10-phenanthroline (phen)/or 2,2' bipyridine (bpy), nih=2-hydroxy-1-naphthaldehyde isonicotinoyl hydrazone, n=2 or 1 and x=3 or 2) have been synthesized and characterized by elemental analysis, magnetic, IR and (1)H NMR spectral data.(More)
The function F includes the use of four S-boxes, each of size 8 x 32, the left circular rotation operation and four operation functions that vary depending on the round number. We label these operation functions as f1i, f2i, f3i and f4i (Fig. 2). We use I to refer to the intermediate 32-bit value after the left circular rotation function and the labels Ia,(More)
Two classes of compounds, thiocarbamates 1 and triazoles 2, have been identified as HIV RT RNase H inhibitors using a novel FRET-based HTS assay. The potent analogs in each series exhibited selectivity and were active in cell-based assays. In addition, saturable, 1:1 stoichiometric binding to target was established and time of addition studies were(More)
Over 195 4-alkyl and 4,4-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives were synthesized, utilizing microwave accelerated synthesis, for evaluation as new inhibitors of bacterial cell wall biosynthesis. Many of them demonstrated good activity against MurB in vitro and low MIC values against gram-positive bacteria, particularly(More)
BACKGROUND RFI-641, a small dendrimer-like compound, is a potent and selective inhibitor of respiratory syncytial virus (RSV), which is currently a clinical candidate for the treatment of upper and lower respiratory tract infections caused by RSV. RFI-641 inhibits RSV growth with an IC(50) value of 50 nM and prevents syncytia formation in tissue culture.(More)
A series of 3,5-dioxopyrazolidines was identified as novel inhibitors of UDP-N-acetylenolpyruvylglucosamine reductase (MurB). Compounds 1 to 3, which are 1,2-bis(4-chlorophenyl)-3,5-dioxopyrazolidine-4-carboxamides, inhibited Escherichia coli MurB, Staphyloccocus aureus MurB, and E. coli MurA with 50% inhibitory concentrations (IC50s) in the range of 4.1 to(More)
Modifications of the D-piece carboxylic acid group of the hemiasterlin analog HTI-286 gave tubulin inhibitors which were potent cytotoxic agents in taxol resistant cell lines expressing P-glycoprotein. Amides derived from proline had potency comparable to HTI-286. Reduction of the carboxylic acid to ketones and alcohols or its conversion to acidic(More)
Potassium channels and their associated subunits are important contributors to electrical excitability in many cell types. In this study, a yeast two-hybrid assay was used to identify inhibitors such as a diaryl-urea compound (CL-888) that binds to and modulates the formation of the Kv4/KChIP complex. CL-888 altered the apparent affinity of KChIP1 to(More)