A Novel Class of Dopamine D4 Receptor Ligands Bearing an Imidazoline Nucleus.

abstract：:The breast cancer resistance protein (BCRP/ABCG2) is a member of the ABC transporter superfamily. This protein has a number of physiological functions, including protection of the human body from xenobiotics. The overexpression of BCRP in certain tumor cell lines causes cross-resistance against various drugs used in c...

journal_title：ChemMedChem

authors： Marighetti F,Steggemann K,Hanl M,Wiese M

更新日期：2013-01-01 00:00:00

abstract：:We previously described synapsin III (Syn III) as a synaptic phosphoprotein that controls dopamine release in cooperation with α-synuclein (aSyn). Moreover, we found that in Parkinson's disease (PD), Syn III also participates in aSyn aggregation and toxicity. Our recent observations point to threo-methylphenidate (MPH...

journal_title：ChemMedChem

authors： Casiraghi A,Longhena F,Straniero V,Faustini G,Newman AH,Bellucci A,Valoti E

更新日期：2020-07-20 00:00:00

abstract：:Leishmaniasis is a complex disease caused by over 20 Leishmania species that primarily affects populations with poor socioeconomic conditions. Currently available drugs for treating leishmaniasis include amphotericin B, paromomycin, and pentavalent antimonials, which have been associated with several limitations, such...

journal_title：ChemMedChem

authors： Herrera-Acevedo C,Perdomo-Madrigal C,Muratov EN,Scotti L,Scotti MT

更新日期：2020-12-17 00:00:00

abstract：:In an approach to design drugs with higher affinity for π-π stacking and electrostatic interactions with targeted biomolecules, complexes of the type [{cis-Pt(A)2 (L)}2 -μ-{trans-1,4-dach}](NO3 )4 ((A)2 =(NH3 )2 or ethylenediamine (en), L=quinoline (quin) or benzothiazole (bztz), dach=trans-1,4-diaminocyclohexane) wer...

journal_title：ChemMedChem

authors： Ma ES,Daniel AG,Farrell NP

更新日期：2014-06-01 00:00:00

abstract：:In atomic force microscopy (AFM) a sharp cantilever tip is used to scan surfaces at the atomic level. One further application is force spectroscopy, in which force-distance curves between binding partners located on the cantilever and substrate surface are determined. This requires specifically immobilized molecules. ...

journal_title：ChemMedChem

authors： David R,Erdmann M,Fornof AR,Gaub HE

更新日期：2014-09-01 00:00:00

abstract：:Following the discovery of a type III allosteric modulator of cyclin-dependent kinase 2 (CDK2) characterized by a hexahydrocyclopenta[c]quinolone scaffold, three different series of its derivatives were synthesized and biologically evaluated. Docking of the synthesized compounds into the allosteric pocket of CDK2 allo...

journal_title：ChemMedChem

authors： Carlino L,Christodoulou MS,Restelli V,Caporuscio F,Foschi F,Semrau MS,Costanzi E,Tinivella A,Pinzi L,Lo Presti L,Battistutta R,Storici P,Broggini M,Passarella D,Rastelli G

更新日期：2018-12-20 00:00:00

abstract：:Chemical biology approaches have a long history in the exploration of the G-protein-coupled receptor (GPCR) family, which represents the largest and most important group of targets for therapeutics. The analysis of the human genome revealed a significant number of new members with unknown physiological function which ...

journal_title：ChemMedChem

authors： Jacoby E,Bouhelal R,Gerspacher M,Seuwen K

更新日期：2006-08-01 00:00:00

abstract：:Efavirenz (EFV), an antiretroviral that interacts clinically with co-administered drugs via activation of the pregnane X receptor (PXR), is extensively metabolized by the cytochromes P450. We tested whether its primary metabolite, 8-hydroxyEFV (8-OHEFV) can activate PXR and potentially contribute to PXR-mediated drug-...

journal_title：ChemMedChem

authors： Narayanan B,Lade JM,Heck CJS,Dietz KD,Wade H,Bumpus NN

更新日期：2018-04-06 00:00:00

abstract：:Bacterial infections are becoming increasingly difficult to treat due to the development and spread of antibiotic resistance. Therefore, identifying novel antibacterial targets and new antibacterial agents capable of treating infections by drug-resistant bacteria is of vital importance. The structurally simple yet pot...

journal_title：ChemMedChem

authors： Bionda N,Stawikowski M,Stawikowska R,Cudic M,López-Vallejo F,Treitl D,Medina-Franco J,Cudic P

更新日期：2012-05-01 00:00:00

abstract：:Numerous studies have shown that chalcones are promising scaffolds for the development of new monoamine oxidase-B (MAO-B) inhibitors. As a continuation of our ongoing research into the development of reversible human MAO-B (hMAO-B) inhibitors, two series of twenty chalcones containing electron-donating and electron-wi...

journal_title：ChemMedChem

authors： Mathew B,Uçar G,Mathew GE,Mathew S,Kalatharakkal Purapurath P,Moolayil F,Mohan S,Varghese Gupta S

更新日期：2016-12-16 00:00:00

abstract：:A novel type of oligonucleotide has been developed, characterized by the attachment of a lysyl moiety to a 2'-O-aminohexyl linker. A protected lysine building block was tethered to 2'-O-aminohexyluridine, and the product was converted into the corresponding phosphoramidite. Up to six modified nucleosides were incorpor...

journal_title：ChemMedChem

authors： Winkler J,Gilbert M,Kocourková A,Stessl M,Noe CR

更新日期：2008-01-01 00:00:00

abstract：:The asymmetric synthesis and receptor pharmacology of (1S,2R,3R,5R,6S)-2-amino-3-Hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (+)-9 (HYDIA) and a few of its O-alkylated derivatives are described. The key step of the synthesis utilizes Sharpless' asymmetric dihydroxylation (AD-beta) for the kinetic resolution of ...

journal_title：ChemMedChem

authors： Woltering TJ,Adam G,Huguenin P,Wichmann J,Kolczewski S,Gatti S,Bourson A,Kew JN,Richards G,Kemp JA,Mutel V,Knoflach F

更新日期：2008-02-01 00:00:00

abstract：:A group of acidic nucleosides were synthesized to develop a new class of ribonuclease A (RNase A) inhibitors. Our recent study on carboxymethylsulfonyl-modified nucleosides revealed some interesting results in RNase A inhibition. This positive outcome triggered an investigation of the role played by secondary sugar hy...

journal_title：ChemMedChem

authors： Datta D,Dasgupta S,Pathak T

更新日期：2014-09-01 00:00:00

abstract：:Lysine-specific demethylase 1 (LSD1) is a flavin adenine dinucleotide (FAD)-dependent enzyme that catalyzes the demethylation of histone H3 and regulates gene expression. Because it is implicated in the regulation of diseases such as acute myeloid leukemia, potent LSD1-specific inhibitors have been pursued. Trans-2-ph...

journal_title：ChemMedChem

authors： Niwa H,Sato S,Handa N,Sengoku T,Umehara T,Yokoyama S

更新日期：2020-05-06 00:00:00

abstract：:The NLRP3 inflammasome is an important regulator of the sterile inflammatory response, and its activation by host-derived sterile molecules leads to the intracellular activation of caspase-1, processing of the pro-inflammatory cytokines interleukin-1β (IL-1β)/IL-18, and pyroptotic cell death. Inappropriate activation ...

journal_title：ChemMedChem

authors： Baldwin AG,Tapia VS,Swanton T,White CS,Beswick JA,Brough D,Freeman S

更新日期：2018-02-20 00:00:00

abstract：:Despite improvements in the treatment and prevention of cancer, the number of new diagnoses continues to rise; this has fuelled substantial interest in the development of new and effective chemotherapeutic agents. Compounds of the triazene class, such as dacarbazine, have been used in the clinical management of many c...

journal_title：ChemMedChem

authors： Diana P,Stagno A,Barraja P,Carbone A,Parrino B,Dall'Acqua F,Vedaldi D,Salvador A,Brun P,Castagliuolo I,Issinger OG,Cirrincione G

更新日期：2011-07-04 00:00:00

abstract：:Indolicidin (IR13), a 13-residue antimicrobial peptide from the cathelicidin family, is known to exhibit a broad spectrum of antimicrobial activity against various microorganisms. This peptide inhibits bacterial DNA synthesis resulting in cell filamentation. However, the precise mechanism remains unclear and requires ...

journal_title：ChemMedChem

authors： Ghosh A,Kar RK,Jana J,Saha A,Jana B,Krishnamoorthy J,Kumar D,Ghosh S,Chatterjee S,Bhunia A

更新日期：2014-09-01 00:00:00

abstract：:This paper describes the synthesis, characterisation, and cytotoxicity of a novel trinuclear platinum complex code named TH1. In addition to its activity against human ovarian cancer cell lines: A2780, A2780(cisR), and A2780(ZD0473R), cell uptake, DNA-binding, and the nature of the compound interaction with pBR322 pla...

journal_title：ChemMedChem

authors： Tayyem H,Huq F,Yu JQ,Beale P,Fisher K

更新日期：2008-01-01 00:00:00

abstract：:Cellular chaperones that belong to the heat-shock protein 90 (Hsp90) family are a prerequisite for successful viral propagation for most viruses. The hepatitis C virus (HCV) uses Hsp90 for maturation, folding, and modification of viral proteins. Based on our previous discovery that marine alkaloid analogues with a 4,5...

journal_title：ChemMedChem

authors： Lillsunde KE,Tomašič T,Schult P,Lohmann V,Kikelj D,Tammela P

更新日期：2019-02-05 00:00:00

abstract：:Targeting LRH-1: Virtual screening and molecular modeling were used to identify novel antagonists of liver receptor homolog-1 (LRH-1), an emerging therapeutic target for breast cancer. Hit compounds were synthesized and biologically assayed, and the preliminary results suggest that raloxifene-based analogues, substitu...

journal_title：ChemMedChem

authors： Rey J,Hu H,Kyle F,Lai CF,Buluwela L,Coombes RC,Ortlund EA,Ali S,Snyder JP,Barrett AG

更新日期：2012-11-01 00:00:00

abstract：:(±)-6-Alkyl-2,4-diaminopyrimidine-based inhibitors of bacterial dihydrofolate reductase (DHFR) have been prepared and evaluated for biological potency against Bacillus anthracis and Staphylococcus aureus. Biological studies revealed attenuated activity relative to earlier structures lacking substitution at C6 of the d...

journal_title：ChemMedChem

authors： Nammalwar B,Bourne CR,Bunce RA,Wakeham N,Bourne PC,Ramnarayan K,Mylvaganam S,Berlin KD,Barrow EW,Barrow WW

更新日期：2012-11-01 00:00:00

abstract：:The tropical diseases human African trypanosomiasis, Chagas disease, and the various forms of leishmaniasis are caused by parasites of the family of trypanosomatids. These protozoa possess a unique redox metabolism based on trypanothione and trypanothione reductase (TR), making TR a promising drug target. We report th...

journal_title：ChemMedChem

authors： De Gasparo R,Brodbeck-Persch E,Bryson S,Hentzen NB,Kaiser M,Pai EF,Krauth-Siegel RL,Diederich F

更新日期：2018-05-08 00:00:00

abstract：:Nanoscale materials hold great promise in the therapeutic field. In particular, as carriers or vectors, they help bioactive molecules reach their primary targets. Furthermore, by themselves, certain nanomaterials-regarded as protective-can modulate particular metabolic pathways that are deregulated in pathological sit...

journal_title：ChemMedChem

authors： Bianco A,Muller S

更新日期：2016-01-19 00:00:00

abstract：:2-Azetidinones, commonly known as beta-lactams, are well-known heterocyclic compounds. Herein we described the synthesis and biological evaluation of a series of novel beta-lactams. In vitro inhibition assays against HDAC isoforms showed an interesting isoform-selectivity of these compounds towards HDAC6 and HDAC8. Th...

journal_title：ChemMedChem

authors： Galletti P,Quintavalla A,Ventrici C,Giannini G,Cabri W,Penco S,Gallo G,Vincenti S,Giacomini D

更新日期：2009-12-01 00:00:00

abstract：:Platinum amidine complexes represent a new class of potential antitumor drugs that contain the imino moiety HN=C(sp(2)) bonded to the platinum center. They can be related to the iminoether derivatives, which were recently shown to be the first Pt(II) compounds with a trans configuration endowed with anticancer activit...

journal_title：ChemMedChem

authors： Michelin RA,Sgarbossa P,Sbovata SM,Gandin V,Marzano C,Bertani R

更新日期：2011-07-04 00:00:00

abstract：:ABC, it's easy as 1 2 3! Bioisosteric replacement of the anilide core by an indole moiety considerably increased stability and gave potent and selective ABCG2 (BCRP) inhibitors. Some compounds are superior to the reference substances fumitremorgin C and Ko143 in terms of potency and efficacy and are the most potent AB...

journal_title：ChemMedChem

authors： Bauer S,Ochoa-Puentes C,Sun Q,Bause M,Bernhardt G,König B,Buschauer A

更新日期：2013-11-01 00:00:00

abstract：:Deoxyuridine 5'-triphosphate nucleotidohydrolase (dUTPase) is a potential drug target for malaria. We previously reported some 5'-tritylated deoxyuridine analogues (both cyclic and acyclic) as selective inhibitors of the Plasmodium falciparum dUTPase. Modelling studies indicated that it might be possible to replace th...

journal_title：ChemMedChem

authors： Hampton SE,Baragaña B,Schipani A,Bosch-Navarrete C,Musso-Buendía JA,Recio E,Kaiser M,Whittingham JL,Roberts SM,Shevtsov M,Brannigan JA,Kahnberg P,Brun R,Wilson KS,González-Pacanowska D,Johansson NG,Gilbert IH

更新日期：2011-10-04 00:00:00

abstract：:The Pathogen Box is a 400-strong collection of drug-like compounds, selected for their potential against several of the world's most important neglected tropical diseases, including trypanosomiasis, leishmaniasis, cryptosporidiosis, toxoplasmosis, filariasis, schistosomiasis, dengue virus and trichuriasis, in addition...

journal_title：ChemMedChem

authors： Veale CGL

更新日期：2019-02-19 00:00:00

abstract：:The role of beta-aminovinyl ketones as synthetic intermediates has been well categorised, but recent developments have shown an interesting array of applications and new chemotherapeutic potential, both in the preparation of biologically active heterocycles and as pharmacophores in their own right.Medicinal chemists a...

journal_title：ChemMedChem

authors： Gaber HM,Bagley MC

更新日期：2009-07-01 00:00:00

abstract：:Given its role in the mediation of energy and glucose homeostasis, the G-protein-coupled bile acid receptor 1 (TGR5) is considered a potential target for the treatment of type 2 diabetes mellitus and other metabolic disorders. By thorough analysis of diverse structures of published TGR5 agonists, a hypothetical ligand...

journal_title：ChemMedChem

authors： Zhu J,Ye Y,Ning M,Mándi A,Feng Y,Zou Q,Kurtán T,Leng Y,Shen J

更新日期：2013-07-01 00:00:00