2'-O-Lysylaminohexyl oligonucleotides: modifications for antisense and siRNA.

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：: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：:The cytotoxic activity of a series of 23 new isoerianin derivatives with modifications on both the A and B rings was studied. Several compounds exhibited excellent antiproliferative activity at nanomolar concentrations against a panel of human cancer cell lines. The most cytotoxic compound, isoerianin (3), strongly in...

journal_title：ChemMedChem

authors： Messaoudi S,Hamze A,Provot O,Tréguier B,Rodrigo De Losada J,Bignon J,Liu JM,Wdzieczak-Bakala J,Thoret S,Dubois J,Brion JD,Alami M

更新日期：2011-03-07 00:00:00

abstract：:Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we describe discovery of a dual (OX(1)R/OX(2)R) orexin receptor antagonist featuring a 1,4-diazepane central constraint that blocks orexin signaling in vivo. In telemet...

journal_title：ChemMedChem

authors： Whitman DB,Cox CD,Breslin MJ,Brashear KM,Schreier JD,Bogusky MJ,Bednar RA,Lemaire W,Bruno JG,Hartman GD,Reiss DR,Harrell CM,Kraus RL,Li Y,Garson SL,Doran SM,Prueksaritanont T,Li C,Winrow CJ,Koblan KS,Renger JJ,C

更新日期：2009-07-01 00:00:00

abstract：:The spider polyamine toxins Joro spider toxin-3 (JSTX-3) and Nephila polyamine toxins-1 and -8 (NPTX-1 and NPTX-8) are isolated from the venom of the orb-weaver spider Nephila clavata (Joro spider). They share a high degree of structural resemblance, their aromatic head groups being the only difference, and were recen...

journal_title：ChemMedChem

authors： Xiong XF,Poulsen MH,Hussein RA,Nørager NG,Strømgaard K

更新日期：2014-12-01 00:00:00

abstract：:The gold standard for the treatment of metastatic colorectal cancer consists of combination chemotherapy. Over time, however, the development of chemoresistant tumor clones leads to relapse. It may be possible to overcome oxaliplatin chemoresistance in colorectal cancer cells by exploiting a complex obtained from the ...

journal_title：ChemMedChem

authors： Gandin V,Marzano C,Pelosi G,Ravera M,Gabano E,Osella D

更新日期：2014-06-01 00:00:00

abstract：:Peroxisome proliferator-activated receptors (PPARs) have been studied extensively over the last few decades and have been assessed as molecular targets for the development of drugs against metabolic disorders. A rapid increase in understanding of the physiology and pharmacology of these receptors has occurred, togethe...

journal_title：ChemMedChem

authors： Ammazzalorso A,De Filippis B,Giampietro L,Amoroso R

更新日期：2013-10-01 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：:Src homology 2 (SH2)-domain-mediated interactions with phosphotyrosine (pY)-containing ligands are critical for the regulation of SHP-1 phosphatase activity. Peptides based on a binding site from receptor tyrosine kinase Ros (EGLN-pY2267-MVL, 1) have recently been shown to bind to the SHP-1 N-terminal SH2 domain (N-SH...

journal_title：ChemMedChem

authors： Hampel K,Kaufhold I,Zacharias M,Böhmer FD,Imhof D

更新日期：2006-08-01 00:00:00

abstract：:The design of compounds selective for the MT1 melatonin receptor is still a challenging task owing to the limited knowledge of the structural features conferring selectivity for the MT1 subtype, and only few selective compounds have been reported so far. N-(Anilinoalkyl)amides are a versatile class of melatonin recept...

journal_title：ChemMedChem

authors： Rivara S,Pala D,Lodola A,Mor M,Lucini V,Dugnani S,Scaglione F,Bedini A,Lucarini S,Tarzia G,Spadoni G

更新日期：2012-11-01 00:00:00

abstract：:Discovered as a modulator of the toxic response to environmental pollutants, aryl hydrocarbon receptor (AhR) has recently gained attention for its involvement in various physiological and pathological pathways. AhR is a ligand-dependent transcription factor activated by a large array of chemical compounds, which inclu...

journal_title：ChemMedChem

authors： Dolciami D,Gargaro M,Cerra B,Scalisi G,Bagnoli L,Servillo G,Fazia MAD,Puccetti P,Quintana FJ,Fallarino F,Macchiarulo A

更新日期：2018-02-06 00:00:00

abstract：:A series of cis-configured epoxides and aziridines containing hydrophobic moieties and amino acid esters were synthesized as new potential inhibitors of the secreted aspartic protease 2 (SAP2) of Candida albicans. Enzyme assays revealed the N-benzyl-3-phenyl-substituted aziridines 11 and 17 as the most potent inhibito...

journal_title：ChemMedChem

authors： Degel B,Staib P,Rohrer S,Scheiber J,Martina E,Büchold C,Baumann K,Morschhäuser J,Schirmeister T

更新日期：2008-02-01 00:00:00

abstract：:It has been 25 years since the development of the first efficient HIV-1/AIDS treatment. Scientists now know more about the HIV-1 infection life cycle, and more than 30 antiretroviral drugs have been developed, including HIV-1 fusion inhibitors. Fundamental work was begun in the early 1990s and led to the development o...

journal_title：ChemMedChem

authors： Cai L,Jiang S

更新日期：2010-11-08 00:00:00

abstract：:The tubulin-binding mode of C3- and C15-modified analogues of epothilone A (Epo A) was determined by NMR spectroscopy and computational methods and compared with the existing structural models of tubulin-bound natural Epo A. Only minor differences were observed in the conformation of the macrocycle between Epo A and t...

journal_title：ChemMedChem

authors： Erdélyi M,Navarro-Vázquez A,Pfeiffer B,Kuzniewski CN,Felser A,Widmer T,Gertsch J,Pera B,Díaz JF,Altmann KH,Carlomagno T

更新日期：2010-06-07 00:00:00

abstract：:Greater than the sum of its parts: Artemisinins are currently in phase I-II clinical trials against breast, colorectal and non-small-cell lung cancers. In an attempt to offer increased specificity, a series of hybrid artemisinin-polypyrrole minor groove binder conjugates are described. DNA binding/modelling studies an...

journal_title：ChemMedChem

authors： La Pensée L,Sabbani S,Sharma R,Bhamra I,Shore E,Chadwick AE,Berry NG,Firman J,Araujo NC,Cabral L,Cristiano ML,Bateman C,Janneh O,Gavrila A,Wu YH,Hussain A,Ward SA,Stocks PA,Cosstick R,O'Neill PM

更新日期：2013-05-01 00:00:00

abstract：:Dual inhibition of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO), two key enzymes involved in pro-inflammatory eicosanoid biosynthesis, represents a new strategy for treating inflammatory disorders. Herein we report the discovery of 2,4-thiazolidinedione-based mPGES-1/5-LO dual inhibitors ...

journal_title：ChemMedChem

authors： Lauro G,Terracciano S,Cantone V,Ruggiero D,Fischer K,Pace S,Werz O,Bruno I,Bifulco G

更新日期：2020-03-18 00:00:00

abstract：:alpha,beta-Unsaturated carbonyl compounds as potential drug candidates is a controversial topic since their potential Michael acceptor activity can lead to cell damage and cytotoxicity. Nevertheless, the alpha,beta-unsaturated carbonyl functionality can be employed as a tool to fine tune biological activity by directl...

journal_title：ChemMedChem

authors： Amslinger S

更新日期：2010-03-01 00:00:00

abstract：:The ferrocenyl diphenol complexes 1,1-bis(4'-hydroxyphenyl)-2-ferrocenyl-but-1-ene (1) and 1,2-bis(4'-hydroxyphenyl)-1-ferrocenyl-but-1-ene [(Z)-2], which differ by the relative position of the two phenolic substituents, display dramatically different antiproliferative activities on cancer cells (1 is far more cytotox...

journal_title：ChemMedChem

authors： Tonolo F,Salmain M,Scalcon V,Top S,Pigeon P,Folda A,Caron B,McGlinchey MJ,Toillon RA,Bindoli A,Jaouen G,Vessières A,Rigobello MP

更新日期：2019-10-04 00:00:00

abstract：:Antimicrobial peptides (AMPs) are promising candidates to help circumvent antibiotic resistance, which is an increasing clinical problem. Amino-terminal copper and nickel (ATCUN) binding motifs are known to actively form reactive oxygen species (ROS) upon metal binding. The combination of these two peptidic constructs...

journal_title：ChemMedChem

authors： Libardo MD,Cervantes JL,Salazar JC,Angeles-Boza AM

更新日期：2014-08-01 00:00:00

abstract：:A library of 40,000 compounds was screened for inhibitors of 2-methylerythritol 2,4-cyclodiphosphate synthase (IspF) protein from Arabidopsis thaliana using a photometric assay. A thiazolopyrimidine derivative resulting from the high-throughput screen was found to inhibit the IspF proteins of Mycobacterium tuberculosi...

journal_title：ChemMedChem

authors： Geist JG,Lauw S,Illarionova V,Illarionov B,Fischer M,Gräwert T,Rohdich F,Eisenreich W,Kaiser J,Groll M,Scheurer C,Wittlin S,Alonso-Gómez JL,Schweizer WB,Bacher A,Diederich F

更新日期：2010-07-05 00:00:00

abstract：:The CXCR3 receptor, a class A G protein-coupled receptor (GPCR), is involved in the regulation and trafficking of various immune cells. CXCR3 antagonists have been proposed to be beneficial for the treatment of a wide range of disorders including but not limited to inflammatory and autoimmune diseases. The structure-b...

journal_title：ChemMedChem

authors： Admas TH,Bernat V,Heinrich MR,Tschammer N

更新日期：2016-03-17 00:00:00

abstract：:The therapeutic potential of photoactive CO-releasing molecules (photoCORMs) have called for close examination of the roles of the ligand(s) and the central metal atoms on the overall photochemical labilization of the metal-CO bonds. Along this line, we have synthesized four metal complexes, namely, [MnBr(azpy)(CO)3 ]...

journal_title：ChemMedChem

authors： Chakraborty I,Carrington SJ,Mascharak PK

更新日期：2014-06-01 00:00:00

abstract：:Nucleoside analogues are extensively used as antiviral and anticancer agents. Their efficiency is dependent on their metabolism into the ultimately active nucleoside triphosphates. Often one step or even more in the metabolism of the nucleoside to the triphosphate is inefficient. To overcome this hurdle, prodrugs of t...

journal_title：ChemMedChem

authors： Weinschenk L,Gollnest T,Schols D,Balzarini J,Meier C

更新日期：2015-05-01 00:00:00

abstract：:Selective inhibitors of the protein tyrosine phosphatase SHP2 (src homology region 2 domain phosphatase; PTPN11), an enzyme that is deregulated in numerous human tumors, were generated through a combination of chemical synthesis and structure-based rational design. Seventy pyridazolon-4-ylidenehydrazinyl benzenesulfon...

journal_title：ChemMedChem

authors： Grosskopf S,Eckert C,Arkona C,Radetzki S,Böhm K,Heinemann U,Wolber G,von Kries JP,Birchmeier W,Rademann J

更新日期：2015-05-01 00:00:00

abstract：:The less polar π-surface of protein amide groups is exposed in many receptor binding sites, either as part of the backbone or in Gln/Asn side chains. Using quantum chemical calculations and Protein Data Bank (PDB) searches on model systems, we investigate the energetics and geometric preferences for the stacking on am...

journal_title：ChemMedChem

authors： Harder M,Kuhn B,Diederich F

更新日期：2013-03-01 00:00:00

abstract：:In solution, amphoteric compounds exist in anionic, uncharged, zwitterionic and cationic forms. The importance of zwitterionic drugs is currently under-represented in the literature. Herein, the acid-base parameters, lipophilicity and solubility of such compounds are discussed to deepen the molecular-level understandi...

journal_title：ChemMedChem

authors： Mazák K,Noszál B

更新日期：2020-07-03 00:00:00

abstract：:AFMC-AIMECS meetings are internationally organized biannually by the Asian Federation for Medicinal Chemistry (AFMC) and are focused on recent studies in drug discovery and development both in academia and industry. Member organizations of the AFMC are the Pharmaceutical Society of Japan, the Chinese Pharmaceutical As...

journal_title：ChemMedChem

authors： Olgac A,Yalcin I,Aki-Yalcin E

更新日期：2020-01-07 00:00:00

abstract：:Dihydropyrimidine-based compounds belong to the first discovered inhibitors of the human mitotic kinesin Eg5. Although they are used by many research groups as model compounds for chemical genetics, considerably less emphasis has been placed on the improvement of this type of inhibitor, with the exception of two recen...

journal_title：ChemMedChem

authors： Prokopcová H,Dallinger D,Uray G,Kaan HY,Ulaganathan V,Kozielski F,Laggner C,Kappe CO

更新日期：2010-10-04 00:00:00

abstract：:In the present work, a series of small molecules were designed and synthesized based on structural optimization. A significant improvement in the enzyme inhibitory activity of these compounds was discovered. Moreover, the tested compounds have moderate preference for class I HDACs over HDAC6, as demonstrated by enzyme...

journal_title：ChemMedChem

authors： Zhang L,Zhang Y,Chou CJ,Inks ES,Wang X,Li X,Hou J,Xu W

更新日期：2014-03-01 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