Search Results - "Smith, Emilie D"
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Discovery of Novel 2-Aminobenzamide Inhibitors of Heat Shock Protein 90 as Potent, Selective and Orally Active Antitumor Agents
Published in Journal of medicinal chemistry (23-07-2009)“…A novel class of heat shock protein 90 (Hsp90) inhibitors was developed from an unbiased screen to identify protein targets for a diverse compound library…”
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Synthesis of C-4 Substituted Nicotine Derivatives via an N-Acylpyridinium Salt of (S)-Nicotine
Published in Organic letters (27-10-2005)“…A variety of novel nicotine derivatives were prepared from (S)-nicotine via a two-step sequence. Addition of a cuprate reagent to an N-acylpyridinium salt of…”
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3
Regioselective C-2 and C-6 Substitution of (S)-Nicotine and Nicotine Derivatives
Published in Organic letters (24-11-2005)“…Regioselective deprotonations of (S)-nicotine and derivatives at the C-2 and C-6 positions of the pyridine ring were performed in good to excellent yields…”
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4
Synthesis of Nicotine Derivatives via Reductive Disilylation of (S)-Nicotine
Published in Organic letters (19-01-2006)“…A variety of novel nicotine derivatives were prepared via reductive disilylation of (S)-nicotine. Treatment of nicotine with lithium powder and…”
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5
Design, synthesis and biological evaluation of renin inhibitors guided by simulated annealing of chemical potential simulations
Published in Bioorganic & medicinal chemistry (01-08-2017)“…[Display omitted] We have applied simulated annealing of chemical potential (SACP) to a diverse set of ∼150 very small molecules to provide insights into new…”
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Discovery of novel aminoquinazolin-7-yl 6,7-dihydro-indol-4-ones as potent, selective inhibitors of heat shock protein 90
Published in Bioorganic & medicinal chemistry letters (01-04-2012)“…Compound affinity to Hsp90 in Kd and cellular activities in IC50. A novel class of Hsp90 inhibitors, structurally distinct from previously reported scaffolds,…”
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A six-step synthesis of ( S)-5-ethenyl-3-(1-methyl-2-pyrrolidinyl)pyridine (SIB-1508Y) from ( S)-nicotine
Published in Tetrahedron letters (27-02-2006)“…The anti-Parkinson’s agent SIB-1508Y was prepared in six steps from ( S)-nicotine in 20% overall yield. The strategy involves a regioselective formylation at…”
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8
Application of Chemoproteomics to Drug Discovery: Identification of a Clinical Candidate Targeting Hsp90
Published in Chemistry & biology (30-07-2010)“…A chemoproteomics-based drug discovery strategy is presented that utilizes a highly parallel screening platform, encompassing more than 1000 targets, with a…”
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A new synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397) and activity in a calcium mobilization assay
Published in Bioorganic & medicinal chemistry (15-01-2008)“…A new chiral synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (2,…”
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10
A new synthesis of the ORL-1 antagonist 1-[(3 R,4 R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2 H-benzimidazol-2-one (J-113397) and activity in a calcium mobilization assay
Published in Bioorganic & medicinal chemistry (2008)“…A new chiral synthesis of the ORL-1 antagonist J-113397 was developed. Its in vitro efficacy was determined using an ORL-1 calcium mobilization assay. A new…”
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