Search Results - "Paliwal, Sunil"
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Structural basis of CX-4945 binding to human protein kinase CK2
Published in FEBS letters (03-01-2011)“…Protein kinase CK2 (CK2), a constitutively active serine/threonine kinase, is involved in a variety of roles essential to the maintenance of cellular…”
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Asymmetric Synthesis of 4,4-Disubstituted-2-Imidazoli-dinones: Potent NK1 Antagonists
Published in Organic letters (13-11-2003)“…A highly efficient and practical synthesis of 4,4-Disubstituted-2-Imidazolidinones utilizing a “self-reproduction of the center of chirality” strategy is…”
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Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions
Published in Bioorganic & medicinal chemistry letters (15-02-2006)“…A series of novel five-membered urea derivatives as potent NK1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl…”
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Design and biological characterization of a series of dual mechanism ERK1/2 inhibitors with a Triazolopyridinone core
Published in Chemical biology & drug design (01-04-2023)“…Oncology clinical development programs have targeted the RAS/RAF/MEK/ERK signaling pathway with small molecule inhibitors for a variety of cancers during the…”
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Discovery of ZN-c3, a Highly Potent and Selective Wee1 Inhibitor Undergoing Evaluation in Clinical Trials for the Treatment of Cancer
Published in Journal of medicinal chemistry (09-09-2021)“…Wee1 inhibition has received great attention in the past decade as a promising therapy for cancer treatment. Therefore, a potent and selective Wee1 inhibitor…”
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Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors
Published in Cancer discovery (01-07-2013)“…The high frequency of activating RAS or BRAF mutations in cancer provides strong rationale for targeting the mitogen-activated protein kinase (MAPK) pathway…”
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Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology
Published in Bioorganic & medicinal chemistry letters (15-06-2018)“…[Display omitted] •Discovery of potent, selective and orally bioavailable ERK inhibitor for oncology.•Synthesis of tert 3-(S)thiomethyl pyrrolidine based ERK…”
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MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology
Published in ACS medicinal chemistry letters (12-07-2018)“…The emergence and evolution of new immunological cancer therapies has sparked a rapidly growing interest in discovering novel pathways to treat cancer. Toward…”
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Thermally stimulated current and electrical conduction in metal (1)-ethyl cellulose-metal (1)/(2) systems
Published in Bulletin of materials science (01-06-1998)“…Depolarization current characteristics of solution grown pure ethyl cellulose (EC) films of about 20µm thickness have been studied as a function of electrode…”
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Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation
Published in ACS medicinal chemistry letters (11-06-2015)“…IRAK4 is a critical upstream kinase in the IL-1R/TLR signaling pathway. Inhibition of IRAK4 is hypothesized to be beneficial in the treatment of autoimmune…”
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Structure-based drug design of clinical compound MK-8353, a novel inhibitor of ERK
Published in Acta crystallographica. Section A, Foundations and advances (20-07-2018)“…Abstract only…”
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Discovery of a series of potent, orally active α,α-disubstituted piperidine NK1 antagonists
Published in Bioorganic & medicinal chemistry letters (01-11-2010)Get full text
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Discovery of a series of potent, orally active alpha , alpha -disubstituted piperidine NK sub(1 antagonists)
Published in Bioorganic & medicinal chemistry letters (01-11-2010)“…Modification of prototype NK sub(1 antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be…”
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Cyclobutane derivatives as potent NK1 selective antagonists
Published in Bioorganic & medicinal chemistry letters (15-07-2006)“…A series of novel cyclobutane derivatives as potent and selective NK1 receptor antagonists is described. Several compounds in this series exhibited high in…”
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Discovery of a series of potent, orally active α,α-disubstituted piperidine NK 1 antagonists
Published in Bioorganic & medicinal chemistry letters (2010)“…Modification of prototype NK 1 antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent…”
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Cyclic urea derivatives as potent NK1 selective antagonists
Published in Bioorganic & medicinal chemistry letters (01-09-2005)“…A series of novel five- and six-membered ring urea derivatives have been described as potent and selective NK1 receptor antagonists. Several compounds in this…”
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Discovery of a novel, potent and orally active series of γ-lactams as selective NK1 antagonists
Published in Bioorganic & medicinal chemistry letters (15-07-2008)“…Strategic replacement of the nitrogen of the lead compound 1 in the original cyclic urea series with a carbon resulted in the discovery of a novel, potent and…”
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Discovery of a novel, potent and orally active series of gamma -lactams as selective NK sub(1) antagonists
Published in Bioorganic & medicinal chemistry (01-07-2008)“…Strategic replacement of the nitrogen of the lead compound 1 in the original cyclic urea series with a carbon resulted in the discovery of a novel, potent and…”
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Discovery of a novel, potent and orally active series of γ-lactams as selective NK 1 antagonists
Published in Bioorganic & medicinal chemistry letters (2008)“…Replacement of nitrogen of the cyclic urea lead 1 with a carbon led to identification of a more potent and orally efficacious γ-lactam series of selective NK 1…”
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