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Crystal structure of calsequestrin from rabbit skeletal muscle sarcoplasmic reticulum
Calsequestrin, the major Ca2+ storage protein of muscle, coordinately binds and releases 40–50 Ca2+ ions per molecule for each contraction-relaxation cycle by an uncertain mechanism. We haveExpand
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Tacrine-ferulic acid-nitric oxide (NO) donor trihybrids as potent, multifunctional acetyl- and butyrylcholinesterase inhibitors.
In search of multifunctional cholinesterase inhibitors as potential anti-Alzheimer drug candidates, tacrine-ferulic acid-NO donor trihybrids were synthesized and tested for their cholinesteraseExpand
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Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.
The phosphoinositide 3-kinase (PI3K) family catalyzes the ATP-dependent phosphorylation of the 3'-hydroxyl group of phosphatidylinositols and plays an important role in cell growth and survival.Expand
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Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.
Transient receptor potential vanilloid 1 (TRPV1) channel antagonists may have clinical utility for the treatment of chronic nociceptive and neuropathic pain. We recently advanced a TRPV1 antagonist,Expand
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Discovery of a novel acetylcholinesterase inhibitor by structure-based virtual screening techniques.
Acetylcholinesterase (AChE) is considered to be one of the most important targets for the treatment of Alzheimer's disease (AD). Previously our group has reported a series of tacrine-based hybrids asExpand
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Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.
N-(6-(6-Chloro-5-(4-fluorophenylsulfonamido)pyridin-3-yl)benzo[d]thiazol-2-yl)acetamide (1) is a potent and efficacious inhibitor of PI3Kα and mTOR in vitro and in vivo. However, in hepatocyte and inExpand
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Tacrine–Flurbiprofen Hybrids as Multifunctional Drug Candidates for the Treatment of Alzheimer's Disease
Five tacrine–flurbiprofen hybrid compounds (3a–e) were synthesized as multi‐target‐directed compounds for the treatment of Alzheimer's disease. Compared to tacrine, two compounds (3d and 3e) showedExpand
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Design, synthesis and evaluation of tacrine-flurbiprofen-nitrate trihybrids as novel anti-Alzheimer's disease agents.
To search for multifunctional anti-Alzheimer's disease (AD) agents with good safety, the previously synthesized tacrine-flurbiprofen hybrids 1a and 1b were modified into tacrine-flurbiprofen-nitrateExpand
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The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.
Based on lead compound 1, which was discovered from a high-throughput screen, a series of PI3Kα/mTOR inhibitors were evaluated that contained an imidazo[1,2-a]pyridine as a core replacement for theExpand
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NO-donating tacrine derivatives as potential butyrylcholinesterase inhibitors with vasorelaxation activity.
  • Y. Chen, J. Sun, +4 authors Y. Zhang
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 1 June 2013
To search for potent anti-Alzheimer's disease (AD) agents with multifunctional effects, 12 NO-donating tacrine-flurbiprofen hybrid compounds (2a-l) were synthesized and biologically evaluated. It wasExpand
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