Search Results - "Chaudhary, Inder"
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A systematic review and activation likelihood estimation meta-analysis of fMRI studies on arousing or wake-promoting effects in Buddhist meditation
Published in Frontiers in psychology (27-10-2023)“…Conventional Buddhist texts illustrate meditation as a condition of relaxed alertness that must fend against extreme hypoarousal (sleep, drowsiness) and…”
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Antitumor Efficacy of PKI-587, a Highly Potent Dual PI3K/mTOR Kinase Inhibitor
Published in Clinical cancer research (15-05-2011)“…The aim of this study was to show preclinical efficacy and clinical development potential of PKI-587, a dual phosphoinositide 3-kinase (PI3K)/mTOR inhibitor…”
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Bis(morpholino-1,3,5-triazine) Derivatives: Potent Adenosine 5′-Triphosphate Competitive Phosphatidylinositol-3-kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of Compound 26 (PKI-587), a Highly Efficacious Dual Inhibitor
Published in Journal of medicinal chemistry (25-03-2010)“…The PI3K/Akt signaling pathway is a key pathway in cell proliferation, growth, survival, protein synthesis, and glucose metabolism. It has been recognized…”
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Hybrid Inhibitors of Phosphatidylinositol 3-Kinase (PI3K) and the Mammalian Target of Rapamycin (mTOR): Design, Synthesis, and Superior Antitumor Activity of Novel Wortmannin−Rapamycin Conjugates
Published in Journal of medicinal chemistry (14-01-2010)“…Hyperactivation of the PI3K/AKT/mTOR signaling pathway is common in cancer, and PI3K and mTOR act synergistically in promoting tumor growth, survival, and…”
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PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors
Published in Cancer biology & therapy (01-05-2005)“…Deregulated phosphatidylinositol 3-kinase (PI3K) signaling pathway is widely implicated in tumor growth and resistance to chemotherapy. While a strong…”
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A Pharmacokinetic Study of Methylphenidate Hydrochloride Multilayer Extended-Release Capsules (Aptensio XR®) in Preschool-Aged Children with Attention-Deficit/Hyperactivity Disorder
Published in Paediatric drugs (01-10-2020)“…Objective This was a single-dose, one-period, multicenter, pharmacokinetic (PK) study to evaluate the PK of methylphenidate (MPH) hydrochloride multilayer…”
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HCV796: A selective nonstructural protein 5B polymerase inhibitor with potent anti‐hepatitis C virus activity In Vitro, in mice with chimeric human livers, and in humans infected with hepatitis C virus
Published in Hepatology (Baltimore, Md.) (01-03-2009)“…Anti‐hepatitis C virus (HCV) drug development has been challenged by a lack of experience with inhibitors inclusive of in vitro, animal model, and clinical…”
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Lead Optimization of N-3-Substituted 7-Morpholinotriazolopyrimidines as Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of PKI-402
Published in Journal of medicinal chemistry (28-01-2010)“…Herein we describe the identification and lead optimization of triazolopyrimidines as a novel class of potent dual PI3K/mTOR inhibitors, resulting in the…”
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PKI-179: An orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor
Published in Bioorganic & medicinal chemistry letters (01-10-2010)“…A series of mono-morpholino 1,3,5-triazine derivatives ( 8a– 8q) bearing a 3-oxa-8-azabicyclo[3.2.1]octane were prepared and evaluated for PI3-kinase/mTOR…”
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2,4-Diamino-quinazolines as inhibitors of β-catenin/Tcf-4 pathway: Potential treatment for colorectal cancer
Published in Bioorganic & medicinal chemistry letters (01-09-2009)“…The synthesis and SAR of a series of 2,4-diamino-quinazoline derivatives as β-catenin/Tcf-4 inhibitors are described. The synthesis and SAR of a series of…”
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SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models
Published in Cancer research (Chicago, Ill.) (15-06-2005)“…Src up-regulation is a common event in human cancers. In colorectal cancer, increased Src levels are an indicator of poor prognosis, and progression to…”
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Cytochrome P450 2B enzyme (CYP2B) induction defect following phenobarbital treatment in the fa/fa Zucker rat: molecular characterization
Published in Archives of biochemistry and biophysics (01-06-1993)“…The present study describes the mechanism of the dampened induction of the CYP2B1 and CYP2B2 genes following phenobarbital treatment in the phenotypically…”
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13
Application of Quantitative NMR in Pharmacological Evaluation of Biologically Generated Metabolites: Implications in Drug Discovery
Published in Drug metabolism and disposition (2011)“…It is important to gain an understanding of the pharmacological activities of metabolite(s) of compounds in development, especially if they are found in…”
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Multimodal biomarker investigation on efficacy and mechanism of action for the mammalian target of rapamycin inhibitor, temsirolimus, in a preclinical mammary carcinoma OncoMouse model: a translational medicine study in support for early clinical development
Published in The Journal of pharmacology and experimental therapeutics (01-11-2011)“…The mammalian target of rapamycin (mTOR) has proven to be a valid therapeutic target in a number of human cancers, and it is a candidate for clinical trials in…”
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Determination of pharmacokinetic values of calicheamicin-antibody conjugates in mice by plasmon resonance analysis of small (5 μl) blood samples
Published in Cancer chemotherapy and pharmacology (01-05-2008)“…Purpose The present study aims to establish a method that provides fast, precise and reproducible pharmacokinetic (PK) parameters of antibody-calicheamicin…”
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Design and Synthesis of Novel Diaminoquinazolines with in Vivo Efficacy for β-Catenin/T-Cell Transcriptional Factor 4 Pathway Inhibition
Published in Journal of medicinal chemistry (28-01-2010)“…We are introducing a novel series of 2,4-diaminoquinazolines as β-catenin/Tcf4 inhibitors which were identified by ligand-based design. Here we elucidate the…”
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Abstract 1677: Epithelial hyperplasia induced by a selective B-Raf inhibitor, WYE-130600
Published in Cancer research (Chicago, Ill.) (15-04-2010)“…Abstract The Raf-MEK-ERK signaling pathway is critical for cell survival, growth, proliferation and tumorigenesis. The RAF kinases, ARAF, BRAF and CRAF, are…”
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Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-05-2010)“…The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC 50 values of 2.1 and 58 nM, respectively, had…”
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4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors
Published in Bioorganic & medicinal chemistry (15-10-2008)“…A series of 7-alkenyl substituted 4-anilino-3-quinolinecarbonitriles were prepared and evaluated as MEK1 kinase inhibitors. One analog (R = H, NR 1R 2 =…”
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Pegylated Wortmannin and 17-Hydroxywortmannin Conjugates as Phosphoinositide 3-Kinase Inhibitors Active in Human Tumor Xenograft Models
Published in Journal of medicinal chemistry (23-02-2006)“…Phosphoinositide 3-kinase (PI3K) is an important target for cancer chemotherapy due to the deregulation of its signaling pathway in a wide spectrum of human…”
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