Anticancer profile of a series of gold(III) (2-phenyl)pyridine complexes.

abstract：:The disruption of aberrant protein-protein interactions (PPIs) with synthetic agents remains a challenging goal in contemporary medicinal chemistry but some progress has been made. One such dysregulated PPI is that between the anti-apoptotic Bcl-2 proteins, including myeloid cell leukemia-1 (Mcl-1), and the α-helical ...

journal_title：ChemMedChem

authors： Drennen B,Scheenstra JA,Yap JL,Chen L,Lanning ME,Roth BM,Wilder PT,Fletcher S

更新日期：2016-04-19 00:00:00

abstract：:Metalloproteinases of the astacin family are drawing ever increasing attention as potential drug targets. However, knowledge regarding inhibitors thereof is limited in most cases. Crucial for the development of metalloprotease inhibitors is high selectivity, to avoid side effects brought about by inhibition of off-tar...

journal_title：ChemMedChem

authors： Tan K,Jäger C,Schlenzig D,Schilling S,Buchholz M,Ramsbeck D

更新日期：2018-08-20 00:00:00

abstract：:Oxoisoaporphine alkaloids are a family of oxoisoquinoline-derived alkaloids that were first isolated from the rhizome of Menispermum dauricum DC. (Menispermaceae). It has been demonstrated that oxoisoaporphine alkaloids possess various biological properties, such as cholinesterase and β-amyloid inhibition, acting as a...

journal_title：ChemMedChem

authors： Zhang J,Chen L,Sun J

更新日期：2018-07-06 00:00:00

abstract：:An efficient stereocontrolled synthesis afforded alkoxymethylenephosphonate (MP) analogues of lysophosphatidic acid (LPA) and phosphatidic acid (PA). The pharmacological properties of MP-LPA and MP-PA analogues were characterized for LPA receptor subtype-specific agonist and antagonist activity using Ca(2+)-mobilizati...

journal_title：ChemMedChem

authors： Gajewiak J,Tsukahara R,Tsukahara T,Fujiwara Y,Yu S,Lu Y,Murph M,Mills GB,Tigyi G,Prestwich GD

更新日期：2007-12-01 00:00:00

abstract：:N-Acylethanolamine acid amidase (NAAA) is a cysteine amidase that preferentially hydrolyzes saturated or monounsaturated fatty acid ethanolamides (FAEs), such as palmitoylethanolamide (PEA) and oleoylethanolamide (OEA), which are endogenous agonists of nuclear peroxisome proliferator-activated receptor-α (PPAR-α). Com...

journal_title：ChemMedChem

authors： Vitale R,Ottonello G,Petracca R,Bertozzi SM,Ponzano S,Armirotti A,Berteotti A,Dionisi M,Cavalli A,Piomelli D,Bandiera T,Bertozzi F

更新日期：2014-02-01 00:00:00

abstract：:The present work describes some recent approaches to novel 3-oxabicyclo[3.2.0]heptane-type nucleosides structurally similar to the potent anti-HIV agent stavudine (d4T). To gain knowledge at the molecular level relevant for further synthetic designs, the lack of activity of these compounds was investigated by computat...

journal_title：ChemMedChem

authors： Figueras A,Miralles-Llumà R,Flores R,Rustullet A,Busqué F,Figueredo M,Font J,Alibés R,Maréchal JD

更新日期：2012-06-01 00:00:00

abstract：:P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a major obstacle for successful cancer chemotherapy. Based on our previous study, 17 novel compounds with the 6,7-dimethoxy-2-{2-[4-(1H-1,2,3-triazol-1-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinoline scaffold were designed and synthesized. Among them, 2-[(1-...

journal_title：ChemMedChem

authors： Liu B,Qiu Q,Zhao T,Jiao L,Li Y,Huang W,Qian H

更新日期：2015-02-01 00:00:00

abstract：:3,6-Dimethyl-1,2,4,5-tetrazine-1,4-dicarboxamide derivatives were synthesized, and their structures were confirmed by single-crystal X-ray diffraction. This reaction yields the 1,4-dicarboxamide derivatives rather than the 1,2-dicarboxamide derivatives. Their in vitro antitumor activities were evaluated against SGC-79...

journal_title：ChemMedChem

authors： Rao GW,Guo YM,Hu WX

更新日期：2012-06-01 00:00:00

abstract：:A synthetic concept is presented that allows the construction of peptide isostere libraries through polymer-supported C-acylation reactions. A phosphorane linker reagent is used as a carbanion equivalent; by employing MSNT as a coupling reagent, the C-acylation can be conducted without racemization. Diastereoselective...

journal_title：ChemMedChem

authors： Weik S,Luksch T,Evers A,Böttcher J,Sotriffer CA,Hasilik A,Löffler HG,Klebe G,Rademann J

更新日期：2006-04-01 00:00:00

abstract：:The Cdc25 dual specificity phosphatases have central roles in coordinating cellular signalling processes and cell proliferation. It has been reported that an improper amplification or activation of these enzymes is a distinctive feature of a number of human cancers, including breast cancers. Thus, the inhibition of Cd...

journal_title：ChemMedChem

authors： Lavecchia A,Cosconati S,Limongelli V,Novellino E

更新日期：2006-05-01 00:00:00

abstract：:Natural products containing the α,β-unsaturated δ-lactone skeleton have been shown to possess a variety of biological activities. The natural product (-)-tarchonanthuslactone (1) possessing this privileged scaffold is a popular synthetic target, but its biological activity remains underexplored. Herein, the total synt...

journal_title：ChemMedChem

authors： Toneto Novaes LF,Martins Avila C,Pelizzaro-Rocha KJ,Vendramini-Costa DB,Pereira Dias M,Barbosa Trivella DB,Ernesto de Carvalho J,Ferreira-Halder CV,Pilli RA

更新日期：2015-10-01 00:00:00

abstract：:The consumption of Brassica vegetables provides beneficial effects through organic isothiocyanates (ITCs), products of the enzymatic hydrolysis of glucosinolate secondary metabolites. The ITC l-sulforaphane (l-SFN) is the principle agent in broccoli that demonstrates several modes of anticancer action. While the antic...

journal_title：ChemMedChem

authors： Anderson RH,Lensing CJ,Forred BJ,Amolins MW,Aegerter CL,Vitiello PF,Mays JR

更新日期：2018-08-20 00:00:00

abstract：:Protein disulfide isomerase (PDI) is overexpressed in glioblastoma, the most aggressive form of brain cancer, and folds nascent proteins responsible for the progression and spread of the disease. Herein we describe a novel nanomolar PDI inhibitor, pyrimidotriazinedione 35G8, that is toxic in a panel of human glioblast...

journal_title：ChemMedChem

authors： Kyani A,Tamura S,Yang S,Shergalis A,Samanta S,Kuang Y,Ljungman M,Neamati N

更新日期：2018-01-22 00:00:00

abstract：:β-Alanyl-D-histidine (D-CAR, the enantiomer of the natural dipeptide carnosine) is a selective and potent sequestering agent of reactive carbonyl species (RCS) that is stable against carnosinase, but is poorly absorbed in the gastrointestinal tract. Herein we report a drug discovery approach aimed at increasing the or...

journal_title：ChemMedChem

authors： Orioli M,Vistoli G,Regazzoni L,Pedretti A,Lapolla A,Rossoni G,Canevotti R,Gamberoni L,Previtali M,Carini M,Aldini G

更新日期：2011-07-04 00:00:00

abstract：:Compound 11 (3-(benzyloxy)-1'-methyl-1'-azonia-4H-1'-azaspiro[isoxazole-5,3'-bicyclo[2.2.2]octane] iodide) was selected from a previous set of nicotinic ligands as a suitable model compound for the design of new silent agonists of α7 nicotinic acetylcholine receptors (nAChRs). Silent agonists evoke little or no channe...

journal_title：ChemMedChem

authors： Quadri M,Matera C,Silnović A,Pismataro MC,Horenstein NA,Stokes C,Papke RL,Dallanoce C

更新日期：2017-08-22 00:00:00

abstract：:Having recently identified a so-far unexplored area adjacent to the known binding site of allosteric mitogen-activated protein kinase kinase (MEK) inhibitors, we now report an extension of these studies by combining our new side chains with different MEK inhibitor cores in a modular manner. Replacement of the amide he...

journal_title：ChemMedChem

authors： Hartung IV,Pühler F,Neuhaus R,Scholz A,Siemeister G,Geisler J,Hillig RC,von Ahsen O,Hitchcock M

更新日期：2015-12-01 00:00:00

abstract：:Phospholipid bilayers represent a complex, anisotropic environment fundamentally different from bulk oil or octanol, for instance. Even "simple" drug association to phospholipid bilayers can only be fully understood if the slab-of-hydrocarbon approach is abandoned and the complex, anisotropic properties of lipid bilay...

journal_title：ChemMedChem

authors： Alakoskela JM,Vitovic P,Kinnunen PK

更新日期：2009-08-01 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：:3-Deazaneplanocin A (DzNep) is a potential epigenetic drug for the treatment of various cancers. DzNep has been reported to deplete histone methylations, including oncogenic EZH2 complex, giving rise to epigenetic modifications that reactivate many silenced tumor suppressors in cancer cells. Despite its promise as an ...

journal_title：ChemMedChem

authors： Tam EK,Nguyen TM,Lim CZ,Lee PL,Li Z,Jiang X,Santhanakrishnan S,Tan TW,Goh YL,Wong SY,Yang H,Ong EH,Hill J,Yu Q,Chai CL

更新日期：2015-01-01 00:00:00

abstract：:A small library of 17 organoruthenium compounds with the general formula [RuII (fcl)(chel)(L)]n+ (in which fcl=face capping ligand, chel=chelating bidentate ligand, and L=monodentate ligand) were screened for inhibitory activity against cholinesterases and glutathione-S-transferases of human and animal origins. Compou...

journal_title：ChemMedChem

authors： Ristovski S,Uzelac M,Kljun J,Lipec T,Uršič M,Zemljič Jokhadar Š,Žužek MC,Trobec T,Frangež R,Sepčić K,Turel I

更新日期：2018-10-22 00:00:00

abstract：:Many methods have been developed to capture the biological similarity between two compounds for use in drug discovery. A variety of similarity metrics have been introduced, the Tanimoto coefficient being the most prominent. Many of the approaches assume that molecular features or descriptors that do not relate to the ...

journal_title：ChemMedChem

authors： Abdo A,Salim N

更新日期：2009-02-01 00:00:00

abstract：:DNA hypomethylating drugs that act on DNA methyltransferase (DNMT) isoforms are promising anticancer agents. By using a well-characterized live-cell system to measure DNA methylation revisions (imprints), we characterize olsalazine, an approved anti-inflammatory drug, as a novel DNA hypomethylating agent. The cell-bas...

journal_title：ChemMedChem

authors： Méndez-Lucio O,Tran J,Medina-Franco JL,Meurice N,Muller M

更新日期：2014-03-01 00:00:00

abstract：:The first series of 2'-substituted 2-(3'-carboxybicyclo[1.1.1]pentyl)glycine derivatives, (2R)- and (2S)-(2',2'-dichloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (10) and (11), and 2-(2'-chloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (12) were synthesized and evaluated as mGluR ligands. Compounds 11 and 12 were shown to ...

journal_title：ChemMedChem

authors： Pellicciari R,Filosa R,Fulco MC,Marinozzi M,Macchiarulo A,Novak C,Natalini B,Hermit MB,Nielsen S,Sager TN,Stensbøl TB,Thomsen C

更新日期：2006-03-01 00:00:00

abstract：:To ascertain whether increasing hydrophobicity can enhance the activity of second-generation antisense oligonucleotides (ASOs) in muscle, we investigated the antisense properties of 2'-O-(2S-methoxypropyl)-RNA (2S-MOP)-modified ASOs. Synthesis of the 2S-MOP 5-methyl uridine phosphoramidite was accomplished on a multi-...

journal_title：ChemMedChem

authors： Yu J,Pandey SK,Khatri H,Prakash TP,Swayze EE,Seth PP

更新日期：2014-09-01 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：:Polo-like kinase-2 (Plk-2) has been implicated as the dominant kinase involved in the phosphorylation of α-synuclein in Lewy bodies, which are one of the hallmarks of Parkinson's disease neuropathology. Potent, selective, brain-penetrant inhibitors of Plk-2 were obtained from a structure-guided drug discovery approach...

journal_title：ChemMedChem

authors： Aubele DL,Hom RK,Adler M,Galemmo RA Jr,Bowers S,Truong AP,Pan H,Beroza P,Neitz RJ,Yao N,Lin M,Tonn G,Zhang H,Bova MP,Ren Z,Tam D,Ruslim L,Baker J,Diep L,Fitzgerald K,Hoffman J,Motter R,Fauss D,Tanaka P,Dap

更新日期：2013-08-01 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：: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：:Better control of postprandial hyperglycemia can be achieved by delaying the absorption of glucose resulting from carbohydrate digestion. Because α-amylase initiates the hydrolysis of polysaccharides, the design of α-amylase inhibitors can lead to the development of new treatments for metabolic disorders such as type ...

journal_title：ChemMedChem

authors： Al-Asri J,Gyémánt G,Fazekas E,Lehoczki G,Melzig MF,Wolber G,Mortier J

更新日期：2016-11-07 00:00:00

abstract：:Protein tyrosine phosphatase 1B (PTP1B) is an important target for the treatment of diabetes. A series of thiazolidin-4-one derivatives 8-22 was designed, synthesized and investigated as PTP1B inhibitors. The new molecules inhibited PTP1B with IC50 values in the micromolar range. 5-(Furan-2-ylmethylene)-2-(4-nitrophen...

journal_title：ChemMedChem

authors： Patel AD,Pasha TY,Lunagariya P,Shah U,Bhambharoliya T,Tripathi RKP

更新日期：2020-07-03 00:00:00