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Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: design, synthesis, structural biology, and molecular docking studies.
A series of novel indole-based PPAR agonists is described leading to discovery of 10k, a highly potent PPAR pan-agonist. The structural biology and molecular docking studies revealed that theExpand
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Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.
Utilizing medicinal chemistry design strategies such as benzo splitting and ring expansion, we converted PPARalpha/gamma dual agonist 1 to selective PPARgamma agonists 19 and 20. Compounds 19 and 20Expand
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Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.
By using a cell-based high throughput screening campaign, a novel angelicin derivative 6a was identified to inhibit influenza A (H1N1) virus induced cytopathic effect in Madin-Darby canine kidneyExpand
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Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities.
The synthesis and structure-activity relationship studies of novel indole derivatives as peroxisome proliferator-activated receptor (PPAR) agonists are reported. Indole, a drug-like scaffold, wasExpand
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Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists.
Type 2 diabetes has rapidly reached an epidemic proportion becoming a major threat to global public health. PPAR agonists have emerged as a leading class of oral antidiabetic drugs. We report aExpand
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Inhibition of soil urease activity by amido derivatives of phosphoric and thiophosphoric acids
SummaryA laboratory experiment was conducted to study inhibition of soil urease activity by amido derivatives of phosphoric and thiophosphoric acids. Results showed that derivatives with higher amidoExpand
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Masked o-benzoquinones in organic synthesis.
An account of the synthetic utility of masked o-benzoquinones is provided. The inter- and intramolecular Diels-Alder reactions of in situ generated masked o-benzoquinones produced cycloadducts inExpand
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Structure-based drug design of a novel family of PPARgamma partial agonists: virtual screening, X-ray crystallography, and in vitro/in vivo biological activities.
  • I. Lu, C. Huang, +15 authors S. Wu
  • Medicine, Chemistry
  • Journal of medicinal chemistry
  • 7 April 2006
Peroxisome proliferator-activated receptor gamma (PPARgamma) is well-known as the receptor of thiazolidinedione antidiabetic drugs. In this paper, we present a successful example of employingExpand
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Design and synthesis of tetrahydropyridothieno[2,3-d]pyrimidine scaffold based epidermal growth factor receptor (EGFR) kinase inhibitors: the role of side chain chirality and Michael acceptor group
HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11Expand
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Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.
A focused library of furanopyrimidine (350 compounds) was rapidly synthesized in parallel reactors and in situ screened for Aurora and epidermal growth factor receptor (EGFR) kinase activity, leadingExpand
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