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Mirabamides A-D, depsipeptides from the sponge Siliquariaspongia mirabilis that inhibit HIV-1 fusion.
Four new cyclic depsipeptides termed mirabamides A-D (1-4) have been isolated from the marine sponge Siliquariaspongia mirabilis and shown to potently inhibit HIV-1 fusion and demonstrate that these peptides can act at the early stages of HIV- 1 entry. Expand
Mirabamides E-H, HIV-inhibitory depsipeptides from the sponge Stelletta clavosa.
Four new depsipeptides, mirabamides E-H (1-4), and the known depsipeptide mirabamide C (5) have been isolated from the sponge Stelletta clavosa, collected from the Torres Strait. The planarExpand
Celebesides A-C and theopapuamides B-D, depsipeptides from an Indonesian sponge that inhibit HIV-1 entry.
Six new depsipeptides belonging to two different structural classes, termed celebesides A-C and theopapuamides B-D, have been isolated from the marine sponge Siliquariaspongia mirabilis using extensive 2D NMR and ESI-MS/MS techniques. Expand
A comparison of the ability of rilpivirine (TMC278) and selected analogues to inhibit clinically relevant HIV-1 reverse transcriptase mutants
A deeper understanding of how rilpivirine and related compounds interact with the NNRTI binding pocket is provided and should facilitate development of novel inhibitors. Expand
4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a Potent Inhibitor of Bacterial Phosphopantetheinyl Transferase That Attenuates Secondary
2-pyridinyl-N-(4-aryl)piperazine-1-carbothioamides are presented, which exhibit submicromolar inhibition of bacterial Sfp-PPTase with no activity toward the human orthologue and highlight the in vitro absorption, distribution, metabolism, and excretion and in vivo pharmacokinetic profiles of compound 55 to demonstrate the potential utility of this small-molecule inhibitor. Expand
Neopetrosiquinones A and B, sesquiterpene benzoquinones isolated from the deep-water sponge Neopetrosia cf. proxima.
Two new marine-derived sesquiterpene benzoquinones which we designate as neopetrosiquinones A (1) and B (2), have been isolated from a deep-water sponge of the family Petrosiidae. The structures wereExpand
Dequalinium, a New Inhibitor of Mycobacterium tuberculosis Mycothiol Ligase Identified by High-Throughput Screening
The screening protocol described is robust and has enabled the identification of new MshC inhibitors, and the more potent of the 2—namely, dequalinium chloride—inhibits MShC with an IC50 value of 24 ± 1 µM. Expand
Structure activity relationships of human galactokinase inhibitors.
  • L. Liu, M. Tang, +13 authors M. Boxer
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 1 February 2015
A quantitative high-throughput screening campaign was described that identified a single chemotype that was optimized and validated as a GALK inhibitor and offered a novel entry therapy for this disorder. Expand
Synthetic macrolides that inhibit breast cancer cell migration in vitro.
Three of the macrolides have been shown to inhibit 4T1 breast cancer cell migration with low nanomolar to sub-micromolar IC50 values in complementary assays including a quantitative cell migration assay and a semiquantitative wound healing assay. Expand