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Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic
An 1,3-oxybenzylglycine based compound 2 (BMS-687453) was discovered to be a potent and selective peroxisome proliferator activated receptor (PPAR) alpha agonist, with an EC(50) of 10 nM for humanExpand
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Structure-activity relationships of diverse Annonaceous acetogenins against multidrug resistant human mammary adenocarcinoma (MCF-7/Adr) cells.
Fourteen structurally diverse Annonaceous acetogenins, representing the three main classes of bis-adjacent, bis-nonadjacent, and single-THF ring(s), were tested for their ability to inhibit theExpand
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Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents.
By targeting the flap backbone of the BACE1 active site, we discovered 6-dimethylisoxazole-substituted biaryl aminothiazine 18 with 34-fold improved BACE1 inhibitory activity over the lead compoundExpand
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Structure of the complex of trypsin with a highly potent synthetic inhibitor at 0.97 A resolution.
The structure of the complex formed between bovine beta-trypsin and the highly potent synthetic inhibitorExpand
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ABSTRACT Stimuli-responsive hydrogels have attracted much interest recently [1]. In this paper, we report a pH- and electrolyte-responsive hydrogel based on a crosslinked poly(aspartic acid). TheExpand
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Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2':6',2"-, 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives.
  • L. Zhao, T. Kim, +9 authors E. Lee
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 8 October 2001
For the development of new anticancer agents, 2,2':6',2"-, 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumorExpand
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Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
  • Wei Wang, P. Devasthale, +22 authors P. Cheng
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 15 March 2008
A novel class of azetidinone acid-derived dual PPARalpha/gamma agonists has been synthesized for the treatment of diabetes and dyslipidemia. The preferred stereochemistry in this series for bindingExpand
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Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain*
Background: Interleukin-23 mediates pathobiology in many autoimmune disorders. Results: A chemogenomics approach identified small molecule agents that block receptor-mediated activation or tyrosineExpand
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Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.
Investigation of various heterocyclic core isosteres of imidazopyrazines 1 & 2 yielded purine derivatives 3 & 8 as potent and selective BTK inhibitors. Subsequent SAR studies of the purine series ledExpand
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Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.
The design, synthesis and structure-activity relationships of a novel series of N-phenyl-substituted pyrrole, 1,2-pyrazole and 1,2,3-triazole acid analogs as PPAR ligands are outlined. The triazoleExpand
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