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Medicinal Chemistry Scholarly Works: Recent submissions
Now showing items 101-120 of 255
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Chlorinated Withanolides from Withania somnifera
(Elsevier, 2011-12)A chlorinated withanolide, 6α-chloro-5β,17α-dihydroxywithaferin A (1), and nine known withanolides, 6α-chloro-5β-hydroxywithaferin A (2), (22R)-5β-formyl-6β,27-dihydroxy-1-oxo-4-norwith-24-enolide, withaferin A, ... -
Withanolides from Jaborosa caulescens var. bipinnatifida
(Elsevier, 2013-12-05)Two new withanolides 2,3-dihydrotrechonolide A (1) and 2,3-dihydro-21-hydroxytrechonolide A (2) were isolated along with two known withanolides trechonolide A (3) and jaborosalactone 39 (4) from Jaborosa caulescens var. ... -
Structure-based Ligand Design of Novel Human Toll-like Receptor 8 Agonists
(Wiley, 2014-04)Toll-like receptor (TLR)-8 agonists activate adaptive immune responses by inducing robust production of T helper 1-polarizing cytokines, suggesting that TLR8-active compounds may be promising candidate adjuvants. We recently ... -
Involvement of dynorphin and kappa opioid receptor in yohimbine-induced reinstatement of heroin seeking in rats
(Wiley, 2013-06)Although kappa opioid receptor (KOP-r) antagonists are known to reduce reinstatement of cocaine, alcohol and nicotine seeking induced by a variety of stressors, the role of KOP-r in yohimbine-induced reinstatement of heroin ... -
Identification of a Novel “Almost Neutral” Mu Opioid Receptor Antagonist in CHO Cells Expressing the Cloned Human Mu Opioid Receptor
(Wiley, 2010-04)The basal (constitutive) activity of G protein-coupled receptors allows for the measurement of inverse agonist activity. Some competitive antagonists turn into inverse agonists under conditions where receptors are ... -
Targeting of Histone Acetyltransferase p300 by Cyclopentenone Prostaglandin Δ12-PGJ2 through Covalent Binding to Cys1438
(ACS, 2012-02-20)Inhibitors of histone acetyltransferases (HATs) are perceived to treat diseases like cancer, neurodegeneration, and AIDS. On the basis of previous studies, we hypothesized that Cys1438 in the substrate binding site could ... -
Protein Targets of Thioacetamide Metabolites in Rat Hepatocytes
(ACS, 2013-04-15)Thioacetamide (TA) has long been known as a hepatotoxicant whose bioactivation requires S-oxidation to thioacetamide S-oxide (TASO) and then to the very reactive S,S-dioxide (TASO2). The latter can tautomerize to form ... -
Metabolism and Toxicity of Thioacetamide and Thioacetamide SOxide in Rat Hepatocytes
(ACS, 2012-09-17)The hepatotoxicity of thioacetamide (TA) has been known since 1948. In rats, single doses cause centrilobular necrosis accompanied by increases in plasma transaminases and bilirubin. To elicit these effects TA requires ... -
Liver Protein Targets of Hepatotoxic 4-Bromophenol Metabolites
(ACS, 2012-08-20)The hepatotoxicity of bromobenzene (BB) is directly related to the covalent binding of both initially formed epoxide and secondary quinone metabolites to at least 45 different liver proteins. 4-Bromophenol (4BP) is a ... -
Identification of Protein Targets of Reactive Metabolites of Tienilic Acid in Human Hepatocytes
(ACS, 2012-05-21)Tienilic acid (TA) is a uricosuric diuretic that was withdrawn from the market only months after its introduction because of reports of serious incidents of drug-induced liver injury including some fatalities. Its ... -
Covalent Modification of Lipids and Proteins in Rat Hepatocytes, and In Vitro, by Thioacetamide Metabolites
(ACS, 2012-09-17)Thioacetamide (TA) is a well-known hepatotoxin in rats. Acute doses cause centrilobular necrosis and hyperbilirubinemia while chronic administration leads to biliary hyperplasia and cholangiocarcinoma. Its acute toxicity ... -
A C-Terminal Heat Shock Protein 90 Inhibitor Decreases Hyperglycemia-induced Oxidative Stress and Improves Mitochondrial Bioenergetics in Sensory Neurons
(American Chemical Society, 2012-04-06)Diabetic peripheral neuropathy (DPN) is a common complication of diabetes in which hyperglycemia-induced mitochondrial dysfunction and enhanced oxidative stress contribute to sensory neuron pathology. KU-32 is a novobiocin-based, ... -
The Synthesis and Evaluation of Flavone and Isoflavone Chimeras of Novobiocin and Derrubone
(Elsevier, 2010-01-01)The natural products novobiocin and derrubone have both demonstrated Hsp90 inhibition and structure–activity relationships have been established for each scaffold. Given these compounds share several key structural features, ... -
Semisynthetic Neoclerodanes as Kappa Opioid Receptor Probes
(Elsevier, 2012-05-01)Modification of the furan ring of salvinorin A (1), the main active component of Salvia divinorum, has resulted in novel neoclerodane diterpenes with opioid receptor affinity and activity. Conversion of the furan ring to ... -
Preliminary Evaluation of a 3H Imidazoquinoline Library as Dual TLR7/TLR8 Antagonists
(Elsevier, 2011-06-15)Toll-like receptors (TLR) -7 and -8 are thought to play an important role in immune activation processes underlying the pathophysiology of HIV and several clinically important autoimmune diseases. Based on our earlier ... -
Total synthesis and evaluation of 22-(3-azidobenzoyloxy)methyl epothilone C for photoaffinity labeling of β-tubulin
(Elsevier, 2009-06-15)The total synthesis of 22-(3-azidobenzoyloxy)methyl epothilone C is described as a potential photoaffinity probe to elucidate the β-tubulin binding site. A sequential Suzuki-aldol-Yamaguchi macrolactonization strategy was ... -
Synthesis and Preliminary Evaluation Steroidal AntiestrogenGeldanamycin Conjugates
(Elsevier, 2013-06-15)Three novel steroidal antiestrogen-geldanamycin conjugates were prepared using a convergent strategy. The antiestrogenic component utilized the 11β-(4-functionalized-oxyphenyl) estradiol scaffold, while the geldanamycin ... -
Synthesis and biological evaluation of arylated novobiocin analogs as Hsp90 inhibitors
(Elsevier, 2011-12-01)Novobiocin analogs lacking labile glycosidic ether have been designed, synthesized and evaluated for Hsp90 inhibitory activity. Replacement of the synthetically complex noviose sugar with simple aromatic side chains produced ... -
Potent Adjuvantic Activity of a CCR1-agonistic Bis-Quinoline
(Elsevier, 2012-01-01)A bis-quinoline compound, (7-chloro-N-(4-(7-chloroquinolin-4-ylamino)butyl)quinolin-4-amine; RE-660) was found to have C-C chemokine receptor type 1 (CCR1)-agonistic properties.RE-660 displayed strong adjuvantic activity ...