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Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design.
In an effort to develop a novel therapeutic agent aimed at addressing the unmet need of patients with osteoarthritis pain, we set out to develop an inhibitor for autotaxin with excellent potency andExpand
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Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1).
Tricyclic isoxazoles were identified from a screen as a novel class of selective multidrug resistance protein (MRP1) inhibitors. From a screen lead, SAR efforts resulted in the preparation of LYExpand
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Plasmon-Enhanced Photocurrent of Photosynthetic Pigment Proteins on Nanoporous Silver
In a quest to fabricate novel solar energy materials, the high quantum efficiency and long charge separated states of photosynthetic pigment-proteins are being exploited through their directExpand
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Metabolism and disposition of the antifolate LY231514 in mice and dogs.
The metabolism and disposition of LY231514 was studied in mice and dogs. LY231514 is a novel pyrrotopyrimidine-based multi-target antifolate (MTA) showing broad in vivo antitumor activity in mouseExpand
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The future of quantum biology
Biological systems are dynamical, constantly exchanging energy and matter with the environment in order to maintain the non-equilibrium state synonymous with living. Developments in observationalExpand
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Syntheses and activities of sulfur and selenium isosteric substitution analogues of retinol.
The syntheses of sulfur and selenium isosteric substitution analogues of retinol, namely, retinyl phenyl thioether (2b), retinyl phenyl selenoether (2c), and retinyl thioacetate (2e) are described.Expand
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2-Amino-3-substituted-6-[(E)-1-phenyl-2-(N-methylcarbamoyl)vinyl]imidazo[1,2-a]pyridines as a Novel Class of Inhibitors of Human Rhinovirus: Stereospecific Synthesis and Antiviral Activity
A series of 2-amino-3-substituted-6-[(E)-1-phenyl-2-(N-methylcarbamoyl)vinyl]imidazo[1,2-a]pyridines 1a−i, structurally related to Enviroxime and its analogous benzimidazoles, was designed andExpand
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A 3-month evaluation of the efficacy of nedocromil sodium in asthma: a randomized, double-blind, placebo-controlled trial of nedocromil sodium conducted by a Canadian multicenter study group.
Nedocromil sodium is a pyranoquinoline dicarboxylic acid derivative, formulated in a metered-dose inhaler. Because nedocromil sodium has in vitro and in vivo anti-inflammatory properties, it wasExpand
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Cyclohexyl-linked tricyclic isoxazoles are potent and selective modulators of the multidrug resistance protein (MRP1).
Structure-activity relationship (SAR) studies on the tricyclic isoxazole series of MRP1 modulators have resulted in the identification of potent and selective inhibitors containing cyclohexyl-basedExpand
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Synthesis and biological evaluation of novel cryptophycin analogs with modification in the β-alanine region
Structure modification of the β-alanine region (fragment C) of the potent antimitotic agent cryptophycin was investigated. This includes: (1) introduction of substituents at the previouslyExpand
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