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Medicinal Chemistry Scholarly Works: Recent submissions
Now showing items 121-140 of 255
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Novobiocin analogues with second-generation noviose surrogates
(Elsevier, 2013-01-15)Hsp90 is a promising therapeutic target for the treatment of cancer. Novobiocin is the first Hsp90 C-terminal inhibitor ever identified and recent structure-activity relationship studies on the noviose sugar identified ... -
Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors
(Elsevier, 2009-12-15)Bicyclic radester analogues have been synthesized and evaluated for Hsp90 inhibitory activity. These analogues induce concentration-dependent degradation of Hsp90-dependent client proteins with the six-membered bicyclic ... -
Click Chemistry to Probe Hsp90: Synthesis and Evaluation of a Series of Triazole Containing Novobiocin Analogues
(Elsevier, 2010-07-01)A series of triazole-containing novobiocin analogues has been designed, synthesized and their inhibitory activity determined. These compounds contain a triazole ring in lieu of the amide moiety present in the natural ... -
Chemical Methods for the Synthesis and Modification of Neoclerodane Diterpenes
(Elsevier, 2009-09-15)Diterpenes are a structural class of molecules that are derived from four isoprene subunits and are widespread throughout nature. A number of neoclerodane diterpenes have been found to have biological activity but a ... -
Structure–Activity Relationship Studies of Functionally Selective Kappa Opioid Receptor Agonists that Modulate ERK 1/2 Phosphorylation While Preserving G Protein Over βArrestin2 Signaling Bias
(ACS, 2015-08-19)Kappa opioid receptor (KOR) modulation is a promising target for drug discovery efforts due to KOR involvement in pain, depression, and addiction behaviors. We recently reported a new class of triazole KOR agonists that ... -
Modulating Molecular Chaperones Improves Mitochondrial Bioenergetics and Decreases the Inflammatory Transcriptome in Diabetic Sensory Neurons
(ACS, 2015-09-16)We have previously demonstrated that modulating molecular chaperones with KU-32, a novobiocin derivative, ameliorates physiologic and bioenergetic deficits of diabetic peripheral neuropathy (DPN). Replacing the coumarin ... -
Simultaneously Targeting the NS3 Protease And Helicase Activities For More Effective Hepatitis C Virus Therapy
(ACS, 2015-08-21)This study examines the specificity and mechanism of action of a recently reported hepatitis C virus (HCV) non-structural protein 3 (NS3) helicase-protease inhibitor (HPI), and the interaction of HPI with the NS3 protease ... -
Novel withanolides target medullary thyroid cancer through inhibition of both RET phosphorylation and the mammalian target of rapamycin pathway
(Elsevier, 2012-12)Background Despite development of current targeted therapies for medullary thyroid cancer (MTC), long-term survival remains unchanged. Recently isolated novel withanolide compounds from Solanaceae physalis are highly ... -
A novel RET inhibitor with potent efficacy against medullary thyroid cancer in vivo
(Elsevier, 2010-12)Background Most medullary thyroid carcinomas (MTC) recur or progress despite optimal surgical resection. Current targeted-therapies show promise but lack durable efficacy and tolerability. The purpose of this study was ... -
A novel HSP-90 inhibitor with highly selective activity against papillary and anaplastic thyroid cancers
(Elsevier, 2009-12)Background HSP90 is a chaperone protein regulating several client proteins involved in thyroid cancer development. The purpose of this study is to mechanisticially evaluate a novel natural-product HSP90 inhibitor in ... -
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin
(American Chemical Society, 2015-11-25)The dynorphin (Dyn) A analog zyklophin ([N-benzyl-Tyr1-cyclo(D-Asp5,Dap8)]dynorphin A(1-11)NH2) is a kappa opioid receptor (KOR) selective antagonist in vitro, is active in vivo and antagonizes KOR in the CNS after systemic ... -
Development of Glucose Regularted Protein 94-Selective Inhibitors Based on the Bnlm and Radamide Scaffold
(American Chemical Society, 2016-04-14)Glucose regulated protein 94 (Grp94) is the endoplasmic reticulum resident of the heat shock protein 90 kDa (Hsp90) family of molecular chaperones. Grp94 associates with many proteins involved in cell adhesion and signaling, ... -
Total Synthesis and Evaluation of c26-Hydroxyepothilone D Derivatives for Photoaffinity Labeling of β-Tubulin
(American Chemical Society, 2010-01-01)Three photaffinity labeled derivatives of epothilone D were prepared by total synthesis, using efficient novel asymmetric synthesis methods for the preparation of two important synthetic building blocks. The key step for ... -
A tea catechin, epigallocatechin-3-gallate, is a unique modulator of the farnesoid X receptor
(Elsevier, 2012-12-04)Farnesoid X receptor (FXR) is a ligand-activated nuclear receptor and serves as a key regulator to maintain health of the liver and intestine. Bile acids are endogenous ligands of FXR, and there are increasing efforts to ... -
Heat shock response and insulin-associated neurodegeneration
(Elsevier, 2011-12-13)Dysfunctional insulin and insulin-like growth factor-I (IGF-I) signaling contributes to the pathological progression of diabetes, diabetic peripheral neuropathy (DPN), Alzheimer's (AD), Parkinson's (PD) and Huntington's ... -
Total Syntheses of Arylindolizidine Alkaloids (+)-Ipalbidine and (+)-Antofine
(American Chemical Society, 2010-09-03)This paper presents the first application of two recently developed reactions to natural product synthesis. The first method involves a 6-endo-trig cyclization to prepare a versatile chiral enaminone building block. The ... -
Synthesis of Fluorinated Benzophenones, Xanthones, Acridones, and Thioxanthones by Iterative Nucleophilic Aromatic Substitution
(American Chemical Society, 2012-01-06)Fluorination of fluorophores can substantially enhance their photostability and improve spectroscopic properties. To facilitate access to fluorinated fluorophores, bis(2,4,5-trifluorophenyl)methanone was synthesized by ... -
Synthesis of 6- and 7-membered cyclic enaminones: Scope and mechanism
(American Chemical Society, 2010-10-15)Six- and seven-membered cyclic enaminones can be prepared using common, environmentally benign reagents. Amino acids are used as synthetic precursors allowing diversification and the incorporation of chirality. The key ... -
Synthesis and Structure activity relationships of EGCG Analogues, A Recently Identified Hsp90 Inhibitor
(American Chemical Society, 2013-08-16)Epigallocatechin-3-gallate (EGCG), the principal polyphenol isolated from green tea, was recently shown to inhibit Hsp90, however structure-activity relationships for this natural product have not yet been produced. Herein, ... -
Synthesis and Evaluation of Radamide Analogues, A Chimera of Radicicol and Geldanamycin
(American Chemical Society, 2009-07-03)Previously, we reported the Hsp90 inhibitory activity of radamide, an open chain amide chimera of geldanamycin and radicicol. Attempts to further expand upon structure–activity relationships for this class of Hsp90 inhibitors ...