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Medicinal Chemistry Scholarly Works: Recent submissions
Now showing items 181-200 of 255
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Direct Hiyama Cross-Coupling of Enaminones With Triethoxy(aryl)silanes and Dimethylphenylsilanol
(American Chemical Society, 2011-10-21)2,3-Dihydropyridin-4(1H)-ones undergo direct C–H functionalization at C5 in the palladium(II)-catalyzed Hiyama reaction, using triethoxy(aryl)silanes and dimethylphenylsilanol. The reagent CuF2 has a dual role in the ... -
Modulating molecular chaperones improves sensory fiber recovery and mitochondrial function in diabetic peripheral neuropathy
(Elsevier, 2013-05-01)Quantification of intra-epidermal nerve fibers (iENFs) is an important approach to stage diabetic peripheral neuropathy (DPN) and is a promising clinical endpoint for identifying beneficial therapeutics. Mechanistically, ... -
Reinstatement of methamphetamine seeking in male and female rats treated with modafinil and allopregnanolone
(Elsevier, 2013-01-01)Background Sex differences in methamphetamine (METH) use (females>males) have been demonstrated in clinical and preclinical studies. This experiment investigated the effect of sex on the reinstatement of METH-seeking ... -
Human psychopharmacology and dose-effects of salvinorin A, a kappa-opioid agonist hallucinogen present in the plant Salvia divinorum
(Elsevier, 2012-05-01)Salvinorin A is a potent, selective nonnitrogenous kappa opioid agonist and the known psychoactive constituent of Salvia divinorum, a member of the mint family that has been used for centuries by Mazatec shamans of Mexico ... -
Copper-Catalyzed Decarboxylative Trifluoromethylation of Allylic Bromodifluoroacetates
(American Chemical Society, 2013-11)The development of new synthetic fluorination reactions has important implications in medicinal, agricultural and materials chemistries. Given the prevalence and accessibility of alcohols, methods to convert alcohols to ... -
Decarboxylative Fluorination Strategies for Accessing Medicinally-relevant Products
(Bentham Science Publishers, 2015-01-01)Fluorinated organic compounds have a long history in medicinal chemistry, and synthetic methods to access target fluorinated compounds are undergoing a revolution. One powerful strategy for the installation of fluorine-containing ... -
Bioactivity of Turmeric-Derived Curcuminoids and Related Metabolites in Breast Cancer
(Bentham Science Publishers, 2014-01-07)While the chemotherapeutic effect of curcumin, one of three major curcuminoids derived from turmeric, has been reported, largely unexplored are the effects of complex turmeric extracts more analogous to traditional medicinal ... -
Compound Ranking Based on a New Mathematical Measure of Effectiveness Using Time Course Data from Cell-Based Assays
(Bentham Science Publishers, 2013-05-16)The half maximal inhibitory concentration (IC50) has several limitations that make it unsuitable for examining a large number of compounds in cytotoxicity studies, particularly when multiple exposure periods are tested. ... -
Fluorescent Mimics of Cholesterol that Rapidly Bind Surfaces of Living Mammalian Cells
(Royal Society of Chemistry, 2016-10-07)Mammalian cells acquire cholesterol, a critical membrane constituent, through multiple mechanisms. We synthesized mimics of cholesterol, fluorescent N-alkyl-3β-cholesterylamine-glutamic acids, that are rapidly incorporated ... -
Toll-like Receptor-8 Agonistic Activities in C2, C4, and C8 Modified Thiazolo[4,5-c]quinolines
(Royal Society of Chemistry, 2013-02-21)Toll-like receptor (TLR)-8 agonists typified by the 2-alkylthiazolo[4,5-c]quinolin-4-amine (CL075) chemotype are uniquely potent in activating adaptive immune responses by inducing robust production of T helper 1-polarizing ... -
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Role of the Furan in Affinity for Opioid Receptors
(Royal Society of Chemistry, 2009-09-21)Further synthetic modification of the furan ring of salvinorin A (1), the major active component of Salvia divinorum, has resulted in novel neoclerodane diterpenes with opioid receptor affinity and activity. A computational ... -
Zyklophin, a short-acting kappa opioid antagonist, induces scratching in mice
(Elsevier, 2014-03-20)It has been shown previously that norbinaltorphimine (norBNI) and 5΄-guanidinonaltrindole (5΄-GNTI), long-acting kappa opioid receptor (KOPR) antagonists, cause frenzied scratching in mice [1;2]. In the current study, we ... -
Salvinorin A Regulates Dopamine Transporter Function Via A Kappa Opioid Receptor and ERK1/2-Dependent Mechanism
(Elsevier, 2014-11)Salvinorin A (SalA), a selective κ-opioid receptor (KOR) agonist, produces dysphoria and pro-depressant like effects. These actions have been attributed to inhibition of striatal dopamine release. The dopamine transporter ... -
Investigation of the role of βarrestin2 in kappa opioid receptor modulation in a mouse model of pruritus
(Elsevier, 2015-12)The kappa opioid receptor (KOR) is involved in mediating pruritus; agonists targeting this receptor have been used to treat chronic intractable itch. Conversely, antagonists induce an inch response at the site of injection. ... -
Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting
(Elsevier, 2015-12)Differential modulation of kappa opioid receptor (KOR) signaling has been a proposed strategy for developing therapies for drug addiction and depression by either activating or blocking this receptor. Hence, there have ... -
Monohydroxylated metabolites of the K2 synthetic cannabinoid JWH-073 retain intermediate to high cannabinoid 1 receptor (CB1R) affinity and exhibit neutral antagonist to partial agonist activity
(Elsevier, 2012-01-18)K2 and several similar purported “incense products” spiked with synthetic cannabinoids are abused as cannabis substitutes. We hypothesized that metabolism of JWH-073, a prevalent cannabinoid found in K2, contributes to ... -
Synthetic Cell Surface Receptors for Delivery of Therapeutics and Probes
(Elsevier, 2013-06-15)Receptor-mediated endocytosis is a highly efficient mechanism for cellular uptake of membrane-impermeant ligands. Cells use this process to acquire nutrients, initiate signal transduction, promote development, regulate ... -
Withaferin A, a Cytotoxic Steroid from Vassobia breWiflora, Induces Apoptosis in Human Head and Neck Squamous Cell Carcinoma
(Journal of Natural Products, 2010-08-20)As part of a program to discover drug leads from plant biodiversity, the present investigation was undertaken to explore the anticancer potential of compounds derived from selected Latin American plants. Bioassay-guided ... -
Gambogic Acid, a Natural Product Inhibitor of Hsp90
(Journal of Natural Products, 2011-04-12)A high-throughput screening of natural product libraries identified (−)-gambogic acid (1), a component of the exudate of Garcinia harburyi, as a potential Hsp90 inhibitor, in addition to the known Hsp90 inhibitor celastrol ... -
Cytotoxic Withanolide Constituents of Physalis longifolia
(Journal of Natural Products, 2011-11-08)Fourteen new withanolides, 1–14, named withalongolides A–N, respectively, were isolated from the aerial parts of Physalis longifolia together with eight known compounds (15–22). The structures of compounds 1–14 were ...